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SML1272

I-BET762

≥98% (HPLC)

Synonym(s):

(4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, GSK525762, GSK525762A, I-BET

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About This Item

Empirical Formula (Hill Notation):
C22H22ClN5O2
CAS Number:
1260907-17-2
Molecular Weight:
423.90
NACRES:
NA.77
PubChem Substance ID:
329825759
UNSPSC Code:
12352200
MDL number:
MFCD22417091
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +80 to +90°, c = 0.3 in methanol

drug control

regulated under CDSA - not available from Sigma-Aldrich Canada

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

CCNC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(OC)=CC=C3N4C1=NN=C4C)=O

InChI

1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1

InChI key

AAAQFGUYHFJNHI-SFHVURJKSA-N

Gene Information

human ... BRD2(6046), BRD3(8019), BRD4(23476), BRDT(676)

Biochem/physiol Actions

I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.
I-BET762 is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins; synthetic histone mimic.
I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC50 values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000179114
0000166781
0000179114
0000166781
0000101605

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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
Wyce A, et al.
Oncotarget, 4(12), 2419-2419 (2013)
Bromodomains: are readers right for epigenetic therapy?.
Conway S J.
ACS Medicinal Chemistry Letters, 3(9), 691?694-691?694 (2012)
Laura Helminen et al.
Nucleic acids research, 52(2), 625-642 (2023-11-28)
Treatment of prostate cancer relies predominantly on the inhibition of androgen receptor (AR) signaling. Despite the initial effectiveness of the antiandrogen therapies, the cancer often develops resistance to the AR blockade. One mechanism of the resistance is glucocorticoid receptor (GR)-mediated
View All Related Papers

Global Trade Item Number

SKUGTIN
SML1272-25MG04061832825557
SML1272-5MG04061838356932