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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cdc2-like Kinase (CLK)-SM04690
SM04690

Chemical Structure : SM04690

CAS No.: 1467093-03-3

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SM04690 (Adavivint, Lorecivivint, SM-04690, SM 04690)

货号: PC-60504Not For Human Use, Lab Use Only.

Adavivint (Lorecivivint, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro, potently inhibits CLK2 and DYRK1A with IC50 of 5.8 and 26.9 nM, respectively.

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10 mg ￥1280 In stock
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50 mg ￥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Adavivint (Lorecivivint, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro, potently inhibits CLK2 and DYRK1A with IC50 of 5.8 and 26.9 nM, respectively.
SM04690 demonstrates selectivity against a panel of 318 kinases, showes ≥90% inhibition of 7 kinases (out of 318) at 0.5 uM.
SM04690 inhibits CLK- and DYRK1A-mediated signaling in hMSCs and chondrocytes, 2–300-fold more potent than CC-671, TG003, ML167, Leucettine L41, ML315.
SM04690 dose dependently inhibited the CLK-mediated phosphorylation of SRSF4, SRSF5, and SRSF6 in hMSCs and human chondrocytes.
SM04690 induces hMSC differentiation into mature, functional chondrocytes and decreases cartilage catabolic marker levels.
SM04690 significantly improves Osteoarthritis Research Society International (OARSI) histology scores and biomarkers in a rodent OA model.

物理化学性质&存储条件

分子量 505.557
分子式 C29H24FN7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(5-{3-[7-(3-fluorophenyl)-1H-imidazo[4,5-c]pyridin-2-yl]-1H-indazol-5-yl}pyridin-3-yl)-3-methylbutanamide

参考文献

1. Yazici Y, et al. Osteoarthritis Cartilage. 2017 Jul 13. pii: S1063-4584(17)31085-3.
2. Deshmukh V, et al. Osteoarthritis Cartilage. 2017 Sep 6. pii: S1063-4584(17)31167-6.
3. V Deshmukh, et al. Osteoarthritis Cartilage. 2019 Sep;27(9):1347-1360. 

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