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SML1272

Sigma-Aldrich

I-BET762

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C22H22ClN5O2
Número CAS:
1260907-17-2
Peso molecular:
423.90
Número MDL:
MFCD22417091
Código UNSPSC:
12352200
ID de substância PubChem:
329825759
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

powder

atividade óptica

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

controle de medicamentos

regulated under CDSA - not available from Sigma-Aldrich Canada

cor

white to beige

solubilidade

DMSO: 10 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

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

chave InChI

AAAQFGUYHFJNHI-SFHVURJKSA-N

Informações sobre genes

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

Ações bioquímicas/fisiológicas

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.
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.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Escolha uma das versões mais recentes:

Certificados de análise (COA)

Lot/Batch Number
126M4711V
116M4753V
045M4703V

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Bromodomains: are readers right for epigenetic therapy?.
Conway S J.
ACS Medicinal Chemistry Letters, 3(9), 691?694-691?694 (2012)
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
Wyce A, et al.
Oncotarget, 4(12), 2419-2419 (2013)
Francesco Paolo Fiorentino et al.
International journal of molecular sciences, 21(24) (2020-12-20)
Small cell lung cancer (SCLC) is an aggressive type of lung cancer with high mortality that is caused by frequent relapses and acquired resistance. Despite that several target-based approaches with potential therapeutic impact on SCLC have been identified, numerous targeted
Brian Krug et al.
Cancer cell, 35(5), 782-797 (2019-05-16)
High-grade gliomas defined by histone 3 K27M driver mutations exhibit global loss of H3K27 trimethylation and reciprocal gain of H3K27 acetylation, respectively shaping repressive and active chromatin landscapes. We generated tumor-derived isogenic models bearing this mutation and show that it
Marlies Vanden Bempt et al.
Cancer cell, 34(2), 271-285 (2018-08-15)
The NUP214-ABL1 fusion is a constitutively activated tyrosine kinase that is significantly associated with overexpression of the TLX1 and TLX3 transcription factors in T cell acute lymphoblastic leukemia (T-ALL). Here we show that NUP214-ABL1 cooperates with TLX1 in driving T-ALL development

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