SB 431542 CAS: 301836-41-9
MF: C22H16N4O3
MW: 384.39

SB 431542 (CAS 301836-41-9)

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备用名: SB 431542 is also known as TGF-β RI Kinase Inhibitor VI.
应用; SB 431542 is a Potent, selective inhibitor of TGF-βRI, specifically at ALK5 and its relatives ALK4 and ALK7.
CAS号码: 301836-41-9
纯度: ≥98%
分子量: 384.39
分子式: C22H16N4O3
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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SB 431542 is a small molecule that acts as a specific and selective inhibitor of TGF-β (transforming growth factor-β) superfamily type I activin receptor-like kinase (ALK) receptors ALK4, 5, and 7. Renal carcinoma studies have demonstrated that SB 431542 is a selective inhibitor of Smad3 phosphorylation (IC50= 94nM) and TGF-β-1 collagen induced lα1 (col Iα1). It has been reported that SB 431542 does not affect the JNK, ERK, or p38 MAP kinase pathways. SB 431542 has been shown to suppress TGF-β induced growth stimulation in MG63 cells, inhibit the motility and proliferation of glioma cells, and block the phosphorylation and translocation of SMADs. SB 431542 is also known as 4-[4-(1,3-Benzodioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide, TGF-β RI Kinase Inhibitor VI, and ALK inhibitor.


参考文献

1. Laping, N.J., et al. 2002. Mol. Pharmacol. 62: 58-64. PMID: 12065755

2. Inman, G.J., et al. 2002. Mol. Pharmacol. 62: 65-74. PMID: 12065756

3. Matsuyama, S., et al. 2003. Cancer Res. 63: 7791-7798. PMID: 14633705

4. Hjelmeland, M.D., et al. 2004. Mol. Cancer Ther. 3: 737-745. PMID: 15210860

物理状态 :
Solid
溶解度 :
Soluble in DMSO (77 mg/ml at 25° C), ethanol (45 mg/ml at 25° C), DMF (~20 mg/ml), DMSO:PBS (pH 7.2) (1:1) (~ 0.5 mg/ml), and water (<1 mg/ml at 25° C).
保存 :
Store at -20° C
熔点 :
315.72° C (Predicted)
沸点 :
~662.36° C at 760 mmHg (Predicted)
密度 :
~1.4 g/cm3 (Predicted)
折射率 :
n20D 1.68 (Predicted)
IC50 :
TGFβ RII: IC50 = 66 nM (human); TGFβ RI: IC50 = 94 nM; ACTR-IB: IC50 = 140 nM
Ki 数据 :
TGFβ RI: Ki= 17 nM (human); casein kinase Iα: Ki= 100 nM (human); PKAα cat: Ki= >1.26 µM (human); CDK9: Ki= >1.58 µM (human); ARK-1: Ki= >1.58 µM (human)
pK值 :
pKa: 10.14 (Predicted), pKb: 2.24 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
PubChem CID :
MDL 号码 :
MFCD05865244
SMILES :
C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

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PMID: # 31313605  Lin, TC.|Lin, YY.|Hsu, CC.|Yang, YP.|Yang, CH.|Hwang, DK.|Wang, CY.|Liu, YY.|Lo, WL.|Chiou, SH.|Peng, CH.|Chen, SJ.|Chang, YL.| et al. 2019. Cell Transplant. 28: 1345-1357.

PMID: # 29337130  2018. Dev. Biol. 435: 26-40.

PMID: # 29886243  Fujita, M.|Tamano, R.|Yoneda, S.|Omachi, S.|Yogo, E.|Rokushima, M.|Shinohara, S.|Sakaguchi, G.|Hasegawa, M.|Asaki, T.| et al. 2018. Eur J Pharmacol. 833: 263-274.

PMID: # 28775339  Khan, FM. et al. 2017. Nat Commun. 8: 198.

PMID: # 29088702  Hangauer, MJ. et al. 2017. Nature. 551: 247-250.

PMID: # 25893292  Hwangbo, C. et al. 2016. Oncogene. 35: 389-401.

PMID: # 25754222  Caballé-Serrano, J. et al. 2016. Clin Oral Implants Res. 27: 226-32.

PMID: # 26279418  Wang, D. et al. 2015. Cell. Physiol. Biochem. 36: 2093-107.

PMID: # 26269769  Guo, Q. et al. 2015. Am J Cancer Res. 5: 2098-112.

PMID: # 25635683  Arshad, A. et al. 2015. PloS one. 10: e0115447.

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