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

Chemical Structure : TACH101 L-lysine

CAS No.: 2908753-10-4

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TACH101 L-lysine (Zavondemstat, QC8222)

货号: PC-22581Not For Human Use, Lab Use Only.

TACH101 (Zavondemstat, QC8222, TACH 101) L-lysine 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.

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5 mg ￥3980 In stock
10 mg ￥5880 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

TACH101 (Zavondemstat, QC8222, TACH 101) L-lysine 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 577.73
分子式 C32H43N5O5
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

L-lysine compound with (R)-3-(((7-((4-isopropylphenyl)(methyl)amino)chroman-4-yl)methyl)amino)isonicotinic acid (1:1)

参考文献

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

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