GSK 525762A
GSK 525762A
CAS: 1260907-17-2
Molecular Formula: C22H22ClN5O2
GSK 525762A - Names and Identifiers
GSK 525762A - Physico-chemical Properties
| Molecular Formula | C22H22ClN5O2 |
| Molar Mass | 423.9 |
| Density | 1.35 |
| Melting Point | >132°C (dec.) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml) |
| Appearance | powder |
| Color | white to beige |
| pKa | 15.71±0.46(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| In vitro study | I-BET-762 inhibits the binding of the BET (bromine region and additional terminal domain) proteins, BRD2, BRD3 and BRD4, to the tandem bromine region of BET with a Kd of 50.5-61.3 nM, in the FRET assay, a tetra-acetylated H4 peptide was substituted for the BET tandem Bromo region with an IC50 of 32.5-42.5 nM. I-BET-762 occupies the acetyl-lysine binding pocket of the BET protein and inhibits the binding of the BET protein to acetylated histones, thereby disrupting the formation of chromatin complexes essential for inflammatory gene expression. Treatment with I-BET-762 on Day 2 of the differentiation process alters the cytokine production of CD4 T cells, upregulates the expression of some anti-inflammatory gene products, and downregulates the expression of some pro-inflammatory cytokines. I-BET-762 inhibits the BET (bromine region and additional terminal domain) proteins, BRD2, BRD3 and BRD4, binding to the tandem bromine region of BET, K d 50.5-61.3 nM, in the FRET assay, a tetra-acetylated H4 peptide was substituted for the BET tandem Bromo region with an IC50 of 32.5-42.5 nM. I-BET-762 occupies the acetyl-lysine binding pocket of the BET protein and inhibits the binding of the BET protein to acetylated histones, thereby disrupting the formation of chromatin complexes essential for inflammatory gene expression. Treatment with I-BET-762 on Day 2 during differentiation, altered CD4 |
| In vivo study | I-BET-762 protection against lipopolysaccharide-induced endotoxin Shock and bacterial-induced sepsis. Mice were cured by a single I-BET dose 1.5 hours after LPS injection. I-BET twice daily injections for 2 days protected mice from sepsis-induced death. Early I-BET-762 treatment of an experimental autoimmune encephalomyelitis (EAE) mouse model inhibits the ability of Th1 differentiated 2D2 T cells to induce Neurogenic inflammation. I-BET-762 protection against lipopolysaccharide-induced endotoxin Shock and bacteria-induced sepsis. Mice were cured by a single I-BET dose 1.5 hours after LPS injection. I-BET twice daily injections for 2 days protected mice from sepsis-induced death. Early I-BET-762 treatment of an experimental autoimmune encephalomyelitis (EAE) mouse model inhibits the ability of Th1 differentiated 2D2 T cells to induce Neurogenic inflammation. |
GSK 525762A - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.359 ml | 11.795 ml | 23.59 ml |
| 5 mM | 0.472 ml | 2.359 ml | 4.718 ml |
| 10 mM | 0.236 ml | 1.18 ml | 2.359 ml |
| 5 mM | 0.047 ml | 0.236 ml | 0.472 ml |
Last Update：2024-01-02 23:10:35
GSK 525762A - Reference Information
| Biological activity | I-BET-762 is a BET (bromodomain and extra terminal domain) protein inhibitor with an IC50 of about 35 nM, which inhibits the production of pro-inflammatory proteins by macrophages, inhibits acute inflammation, and is highly selective for proteins contained in other bromine binding domains. Molibresib (I-BET-762, GSK525762, GSK525762A) is a BET protein inhibitor. IC50 is about 35 nM in cell-free test. it inhibits the production of pro-inflammatory proteins by macrophages and inhibits acute inflammation. it is highly selective for proteins contained in other bromine binding domains. |
| in vitro study | I-BET-762 inhibit BET (bromine region and additional terminal domain) proteins, BRD2, BRD3 and BRD4, bound to the tandem bromine region of BET, Kd is 50.5-61.3 nM, in FRET analysis, a tetraacetylated H4 peptide displacing the tandem bromine region of BET, IC50 is 32.5-42.5 nM. I-BET-762 occupy the acetyl-lysine binding pocket of BET proteins and inhibit BET protein binding to acetylated histones, thereby disrupting the formation of chromatin complexes essential for inflammatory gene expression. On the 2nd day of differentiation, I-BET-762 treatment was used to change the cytokine production of CD4 T cells, up-regulate the expression of some anti-inflammatory gene products, and down-regulate the expression of some pro-inflammatory cytokines. I-BET-762 inhibits BET (bromine region and additional terminal domain) proteins, BRD2, BRD3 and BRD4, and binds to the tandem bromine region of BET. K d is 50.5-61.3 nM. In FRET analysis, a tetraacetylated H4 peptide in the tandem bromine region of BET is replaced, and IC50 is 32.5-42.5 nM. I-BET-762 occupy the acetyl-lysine binding pocket of BET proteins and inhibit BET protein binding to acetylated histones, thereby disrupting the formation of chromatin complexes essential for inflammatory gene expression. On the 2nd day of differentiation, I-BET-762 was used to change CD4 |
| in vivo study | I-BET-762 protection against lipopolysaccharide-induced endotoxin shock and bacterial-induced sepsis. A single dose of I-BET treatment 1.5 hours after LPS injection cured mice. I-BET was injected twice daily for 2 days to protect mice from death caused by sepsis. Early I-BET-762 treatment of experimental autoimmune encephalomyelitis (EAE) mouse model inhibits the ability of Th1 differentiated 2D2 T cells to induce neuroinflammation. I-BET-762 protection prevents lipopolysaccharide-induced endotoxin shock and bacterial-induced sepsis. A single dose of I-BET treatment 1.5 hours after LPS injection cured mice. I-BET was injected twice daily for 2 days to protect mice from death caused by sepsis. Early I-BET-762 treatment of experimental autoimmune encephalomyelitis (EAE) mouse model inhibits the ability of Th1 differentiated 2D2 T cells to induce neuroinflammation. |
| target | TargetValue BET proteins (Cell-free say) 35 nM |
| Target | Value |
| BET proteins (Cell-free assay) | 35 nM |
Last Update：2024-04-09 21:54:55
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View History
GSK 525762A
Hydrogen peroxide
2-Methoxyethyl cyanoacetate
EUPANTOL
PROPARGYL ALCOHOL
γ-庚内酯
Nerol
Rad-E-Cate 16
methyl dichlorophosphite
Sitagliptin phosphate hydrate
Hydrogen peroxide
2-Methoxyethyl cyanoacetate
EUPANTOL
PROPARGYL ALCOHOL
γ-庚内酯
Nerol
Rad-E-Cate 16
methyl dichlorophosphite
Sitagliptin phosphate hydrate