콘텐츠로 건너뛰기
Merck

주요 문서

모든 문서 보기

SML1272

I-BET762

≥98% (HPLC)

동의어(들):

(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

조직 및 계약 가격을 보려면 로그인를 클릭합니다.

크기 선택

보기 변경

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C22H22ClN5O2
CAS 번호:
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
기술 서비스
도움이 필요하신가요? 저희 숙련된 과학자 팀이 도와드리겠습니다.
도움 문의

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)

관련 카테고리

Biochem/physiol Actions

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 is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins; synthetic histone mimic.
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.

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number
0000179114
0000166781
0000179114
0000166781
0000101604

적합한 버전을 찾을 수 없으신가요?

특정 버전이 필요한 경우 로트 번호나 배치 번호로 특정 인증서를 찾을 수 있습니다.

COA 검색

이 제품을 이미 가지고 계십니까?

문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

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
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
모든 관련된 서류 보기

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

고객지원팀으로 연락바랍니다.