SB 431542

한글명:SB 431542

카스 번호301836-41-9

상품명:SB 431542

CBNumberCB5360318

분자식C22H16N4O3

포뮬러 무게384.39

MOL 파일301836-41-9.mol

화학적 성질

녹는점	214 °C(dec.)
끓는 점	662.4±55.0 °C(Predicted)
밀도	1.373
인화점	354.4℃
저장 조건	Sealed in dry,Store in freezer, under -20°C
용해도	DMSO: 10mg/mL, 가용성
물리적 상태	가루
산도 계수 (pKa)	10.14±0.10(Predicted)
색상	노란색
안정성	제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 3개월 동안 보관할 수 있습니다.
InChIKey	FHYUGAJXYORMHI-UHFFFAOYSA-N

위험 및 안전 성명

안전지침서	22-24/25
WGK 독일	3
HS 번호	29349990

그림문자(GHS)

SB 431542 화학적 특성, 용도, 생산

개요
SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 94 nM). It is a less potent antagonist of ALK4 (IC₅₀ = 140 nM) and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer. Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.
정의
ChEBI: A member of the class of benzamides that is 4-(imidazol-2-yl)benzamide carrying additional 1,3-benzodioxol-5-yl and pyridin-2-yl substituents at positions 4 and 5 respectively on the imidazole ring.
일반 설명
A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 μM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC₅₀ = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC₅₀ ≥10 μM in the presence of 10 μM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).
생물학적 활성
Potent and selective inhibitor of the transforming growth factor- β (TGF- β ) type I receptor activin receptor-like kinase ALK5 (IC 50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF- β -induced proliferation of human osteosarcoma cells. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells.

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