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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-TACH101
TACH101

Chemical Structure : TACH101

CAS No.: 1851412-93-5

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TACH101 (Zavondemstat, QC8222, TACH 101)

货号: PC-72259Not For Human Use, Lab Use Only.

TACH101 (Zavondemstat, QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of 80 nM against all four isoforms.

规格 价格 库存 数量
2 mg ￥1980 In stock
5 mg ￥2980 In stock
10 mg ￥4580 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TACH101 (Zavondemstat, QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of 80 nM against all four isoforms.
TACH101 weakly inhibits KDM5 family members with IC50 of 140-400 nM, and shows significantly lower potency against KDM2, KDM3, KDM6, and KDM7 family members.
TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.
Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.
TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

物理化学性质&存储条件

分子量 431.54
分子式 C26H29N3O3
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

4-Pyridinecarboxylic acid, 3-[[[(4R)-3,4-dihydro-7-[methyl[4-(1-methylethyl)phenyl]amino]-2H-1-benzopyran-4-yl]methyl]amino]-

参考文献

1. Chandtip Chandhasin, et al. Anticancer Drugs. 2023 Nov 1;34(10):1122-1131.

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