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Chemical Structure : TACH101
CAS No.: 1851412-93-5
Catalog No.: 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.
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|---|---|---|---|
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| 5 mg | $398 | In stock | |
| 10 mg | $598 | In stock | |
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| 100 mg | Get quote |
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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%.
| M.Wt | 431.54 | |
| Formula | C26H29N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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]- |
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1. Chandtip Chandhasin, et al. Anticancer Drugs. 2023 Nov 1;34(10):1122-1131.
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