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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-TK-129
TK-129

Chemical Structure : TK-129

CAS No.: 3031476-73-7

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TK-129 (TK129)

货号: PC-22358Not For Human Use, Lab Use Only.

TK-129 is a highly potent, selective, and orally efficacious KDM5B ((lysine demethylase 5B, JARID1B) inhibitor with IC50 of 44 nM in homogeneous time-resolved fluorescence assay (HTRF).

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5 mg ￥1180 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4980 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

TK-129 is a highly potent, selective, and orally efficacious KDM5B ((lysine demethylase 5B, JARID1B) inhibitor with IC50 of 44 nM in homogeneous time-resolved fluorescence assay (HTRF).
TK-129 also potently inhibits KDM5A with an IC50 value of 0.079 μM but is less effective toward KDM5C (IC50 = 0.353 μM).
TK-129 increases the expression level of KDM5B substrate H3K4me3 protein in neonatal rat cardiac fibroblasts (NRCFs), with low cytotoxicity.
TK-129 alleviates Ang II-induced activation, migration, and proliferation of myocardial fibroblasts in NRCFs.
TK-129 alleviates myocardial remodeling induced by isoproterenol (ISO) in pathological myocardial remodeling in vivo.

物理化学性质&存储条件

分子量 305.38
分子式 C15H23N5O2
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

(R)-1-Cyclopropyl-3-(1-(3-isopropyl-1H-pyrazole-5-carbonyl)pyrrolidin-3-yl)urea

参考文献

1. Kai Tang, et al. J Med Chem. 2022 Oct 13;65(19):12979-13000.

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