(A) Schematic of the BET Bromodomain proteins and chemical structures. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). At. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Resolution:A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). The imidazoquinolinone 8-position of iBET151 was identified as orienting towards the. 3; Cell. Fig. toronto@thesgc. Its mechanism of action is not fully understood. 6SWO: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD1 (GSK778) PDB ID: 6SWO Download: MMDB ID: 192698: PDB Deposition Date: 2019/9/22: Updated in MMDB: 2021/02: Experimental Method: x-ray diffraction. 61 bulk manufacturing, sourcing and procurement. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. GSK778 Hydrochloride. Applications Products Services Documents Support. Shelf Life: >3 years if stored properly. Obviously, GSK778 reduces the clonogenic capacity of primary human AML cells. GSK778에 대한 모든 정보는 Chemicalbook 에서 조회 할 수 있습니다. GSK778 phenocopies the. $21. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. RVX-297 is a 4-quinazolinone derivative related to RVX-208 with an alkylpyrrolidine side chain off the di-methyl substituted phenyl ring (Fig. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. rednibar) and I. Their affinities for the individual bro-modomains of the BET family were initially determined by TR-FRET (Fig. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Email. Copy Link. Available to order from Sigma-Aldrich. In humans, 61 bromodomains, each composed of ∼110 amino acids forming four antiparallel α helices (αZ, αA, αB, and αC) and two hydrophobic (ZA and BC) loops, in 46 different proteins have been described. ≥98% (HPLC)GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Here, two unexpected findings are reported: (1) SynGRs bearing pan-BET or BD2-selective ligands license transcription at the FXN locus, whereas those bearing BD1-selective ligands do not, and (2) rather than being neutral or inhibitory, an untethered BD1-selective ligand (GSK778) substantively enhances the activity of all active SynGRs. 5 GSK778 (BD1) ↓. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. Available to order from Sigma-Aldrich. BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEINS. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Available to order from Sigma-Aldrich. GSK778. , 2012). GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Safety Information. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Purity : >98% (HPLC)Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 (iBET-BD1) potently inhibits numerous cancer cells. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. K. 22 Early preclinical results demonstrate different phenotypic responses from domain-selective BET inhibitors and reduced toxicity when using pan-BET BD2 selective inhibitors. Fig. All Photos (1) SML3234. Contains a pharmaceutically active ingredient. Gamma (γ) Secretase (GS) Inhibitors. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Copy Link. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. WGK 3. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. CAS No. Copy Link. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from AbMole BioScience. Handling should only be performed by personnel trained and familiar with handling of potent active pharmaceutical ingredients. Cell proliferation outcomes in naïve CD4+ T cell counts following 6 days of culture, for each of the two genotypes under the four treatment conditions (i. SGC Toronto. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride. All Photos (1) Documents. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 4. Selectivity profile of I-BET151, iBET-BD1 (GSK778) and iBET-BD2 (GSK046). Biological Activity：GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 14 Whereas a pan-BET inhibitor impeded differentiation of oligodendrocytes, olinone induced this process. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. SERP Rating Probe GSK778 is in the process of SERP review. KR EN. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. SGC chemical probes are open-access. Related Post. HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 1. Forodesine hydrochloride ≥98% (HPLC); Synonyms: 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one, hydrochloride salt,BCX-1777 HCl,ImmH HCl,Immucillin-H HCl; find Sigma-Aldrich-SML3378 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Copy Link. 1iBET-BD1 (GSK778) Following the initial report of the biological activity of iBET-BD1 and iBET-BD2, 19 Wellaway et al. Copy Link. All Photos (1) Documents. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. GSK778 Hydrochloride. ≥98% (HPLC)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. ≥98% (HPLC)We used the BD1-selective small molecule inhibitor GSK778, which largely phenocopies pan-BET inhibitors, as well as the BD2-selective inhibitor GSK046, which has more limited effects on steady. Available to order from Sigma-Aldrich. Request PDF | A Simple Electrostatic Model for the Hard-Sphere Solute Component of Nonpolar Solvation | We propose a new model for estimating the free energy of forming a molecular cavity in a. Available to order from Sigma-Aldrich. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. For example, whereas a BD1-selective inhibitor (GSK778) showed similar phenocopies of pan BETis in cancers, a BD2-selective inhibitor (GSK046) showed better effectiveness in inflammatory and autoimmune diseases 2. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Safety Information. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. (A) Schematic of the BET bromodomain proteins and chemical structures. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Theoretical Analysis Hodoodo Cat#: H408120 Name: GSK778 CAS#: 2451862-42-1By surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 [26]. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 61: Molecular Formula: C 30 H 33 N 5 O 3. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 5 upper limit of normal (ULN) Total bilirubin < 1. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). CAS No. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Safety Information. 1 ± 0. Email. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). 27, 42. 5 (LPS-PBMC assay) ≤ 10 µM. All Photos (1) Documents. PM EN. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 reduces the production of anti-keyhole limpet. FRAP, BAZ2A: 1000 1-25719566: 10 GSK2801. All Photos (1) SML3234. showed that BD(1)-specific GSK778 phenocopied the effects of pan-BET BRD inhibitors, while GSK046 and its orally bioavailable GSK620 derivative had minimal impact on cell viability while impairing the induction, but not the maintenance, of transcriptional programs [133]. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Catalog No. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. 8300 Cypress Creek Parkway, Suite 450 Houston. gov means it’s official. ksg@ahjnirp. SA EN. 27, 42. Copy Link. Catalog No. I-BET151, GSK778, GSK046 and GSK620 are available from R. iBET-BD1 dihydrochloride . Drug Formulation: This drug may be formulated in DMSO. 9 BRD: BAZ2A/2B: BAZ2-ICR. Applications Products Services Documents Support. Applications Products Services Documents Support. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Open in a separate window. COO/ COA. By Louis Gilman. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Binding free energy predictions suggest that entropy changes, electrostatic interactions, and van der Waals interactions are key factors in the selective binding of BD1 and BD2 by SG3-179, GSK778. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. +86-21-51987688 Crystal structure of GSK778 complexed with BRD4-BD1 (Fig. 포함:구조식 이미지,카스 번호(CAS),분자식,녹는점,끓는 점,밀도. GSK778 Hydrochloride. Phone: +1 510. The two tandem bromodomains of the BET. GSK778. ≥98% (HPLC)Shop Medchemexpress LLC HY-136570 5mg , GSK778 CAS:2451862-42-1 Purity:>98% at Fishersci. GlaxoSmithKline; BRD2, BRD3, BRD4, BRDT (BD2) GSK046; pIC50 = 7. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections Ram K. Many reports have shown that pan BETis, such as JQ1 and iBET762, exhibited no selectivity between BD1 and BD2, but BD1-selective (GSK778) or BD2-selective (GSK046 and ABBV-744) BETis showed. Available to order from Sigma-Aldrich. Th17 driving medium or T cell maintenance medium in the presence of either GSK776 (GSK2794776A - an inactive diastereomer) or GSK778 (GSK2794778A -an inverse agonist of RORC)). GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 33DFTG (TD139) $21. Email. The authors report the development of GSK046 (iBET-BD2), a potent BD2-selective inhibitor with >1000-fold selectivity over BD1. GSK778 Hydrochloride. While GSK789 was less selective (TAF1-BD2 K d = 50 nM and TAF1L-BD2 K d = 398 nM), it. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house Griess assay. VN EN. HR EN. SML3234. SML3234. COO/ COA. Modukuri a,1, Zhifeng Yu , Zhi Tan , Hai Minh Tab,1, Melek Nihan Ucisik a. D5782. Sigma-Aldrich. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516, 63 UMN627, 64 and GSK789. To explore the individual functional. , 2013). Herein,. Available to order from Sigma-Aldrich. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. COO/ COA. iBET-BD1 phenocopies the effects of pan-BET inhibitors in cancer models, whereas iBET-BD2 is predominantly effective in. We would like to show you a description here but the site won’t allow us. GSK778 Hydrochloride. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. g ABBV-744, Fig. described the development of GSK778 (iBET-BD1) and GSK046 (iBET-BD2), the first highly selective small-molecule inhibitors of BET-BD1 and BET-BD2, respectively . Louis Gilman July 17, 2023. GSK778 phenocopies the effects of pan- BET inhibitors in cancer models. All Photos (1) SML3234. 5 (LPS-PBMC assay) <10: 8 GSK620 (BD2) pIC50 = 7. All. 11 - Combustible Solids. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). Apart from BRDs, YEATS family members have been. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 1. GSK778 Hydrochloride. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. ≥98% (HPLC) All Photos (1)MS40224, and GSK77825. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. MR EN. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. They also report the development of GSK620, an orally bioavailable BD2-selective inhibitor, and GSK778 (iBET-BD1), a. SML3234. GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis . 11 - Combustible Solids. Drug Formulation: This drug may be formulated in DMSO. LT EN. Available to order from Sigma-Aldrich. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. $79. 5 mg/dL, except in individuals with Gilbert's syndrome. But, how does GSK778 work on the target? Let’s discuss it in detail. Applications Products Services Documents Support. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. BRDT. BE EN. HY-136570 25mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Preis und Verfügbarkeit anzeigen. COO/ COA. Available to order from Sigma-Aldrich. CAS# 2451862-42-1. Figure 4. Copy Link. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. All Photos (1) Documents. However, recent reports of potent and selective pan-BET BD1 and pan-BET BD2 inhibitors have been reported including ABBV-744, 21 GSK778, and GSK046. COO/ COA. GSK778 phenocopies the. Applications Products Services Documents Support. All Photos (1) SML3234. 61 bulk manufacturing, sourcing and procurement. In recent years, members of the bromodomain and. 33DFTG (TD139) $21. Guanidine hydrochloride; Useful for denaturing proteins and solubilization of inclusion bodies. Cell lysates were separated by SDS-PAGE on [email protected] μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. Available to order from Sigma-Aldrich. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. Available to order from Sigma-Aldrich. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. ([email protected]) and I. AR EN. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Your information is safe with us. Email. Molecular Weight: 511. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. Adequate renal, hepatic, pulmonary and cardiac function defined as: Creatinine clearance (as estimated by Cockcroft Gault) > 60 mL/min. A320. Copy Link. No; GlaxoSmithKlineBy surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 . 00. 6147. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). Products are for research use only. 8902. 5 (LPS-PBMC assay) ≤ 10 µM. K. The two tandem. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. GSK778 reduces the production of anti-keyhole limpet. Last but not the least, GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. Available to order from Sigma-Aldrich. MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. 6SWN, 6SWO, 6SWP, 6SWQ. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. COO/ COA. Sigma-Aldrich. Using these molecules, Gilan et al. Available to order from Sigma-Aldrich. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. ksg@ahjnirp. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. While GSK789 was less selective (TAF1-BD2 K d = 50 nM and TAF1L-BD2 K d = 398 nM), it. GSK778. Copy Link. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK046 (iBET-BD2) es un inhibidor de bromodominio BD2 potente, selectivo y oralmente activo de las proteÍnas BET, con IC50 de 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) y 214 nM (BRDT BD2), respectivamente. ≥98% (HPLC)Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. We would like to show you a description here but the site won’t allow us. 77 The basic structure of BET proteins is comprised of. • GSK778 exhibits >130-fold BD1 selectivity over BD2 due to BD1 Asp144/His433 displacement (Kharenko et al. e. GSK778 (68), yielded by introducing an additional pyrrolidine to compound 19 (Fig. Hazard Description: Toxic. GSK778 Hydrochloride. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Email. FRAP, BAZ2B: 1000 3:. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. 11 - Combustible Solids. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. Available to order from Sigma-Aldrich. Solubility: Soluble in DMSO. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). Applications Products Services Documents Support. Dagrocorat. Copy Link. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Safety Information. Federal government websites often end in . ChemicalBook provide Chemical industry users with GSK778 Boiling point Melting point,GSK778 Density MSDS Formula Use,If You also need to GSK778 Other information,welcome to contact us. (E) Ratio of cell viability in the tumor vs normal is represented in the heat map, where the blue color indicates strong effects in tumor organoids and orange shows pronounced effects in. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. , 1999). The RNA. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 00. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. (A) Schematic of the BET bromodomain proteins and chemical structures. 125 nM (MV-4−11 cells) ≤. TC EN. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. Molecular Formula: C30H33N5O3. SML3168. Copy Link. SML3234. COO/ COA. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Email. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. SML3234. 1. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. S1F. 1B, fig. GSK778 Hydrochloride. 2h 04m.