Chemical Structure : AGPAT4 inhibitor CL26
货号: PC-25223Not For Human Use, Lab Use Only.
AGPAT4 inhibitor CL26 is a potent, isoform-specific, covalent inhibitor of acylglycerol-3-phosphate o-acyltransferase 4 (AGPAT4) inhibitor with IC50 of 795 nM, binds to Cys228 of AGPAT4.
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AGPAT4 inhibitor CL26 is a potent, isoform-specific, covalent inhibitor of acylglycerol-3-phosphate o-acyltransferase 4 (AGPAT4) inhibitor with IC50 of 795 nM, binds to Cys228 of AGPAT4.
CL26 exhihits specificity toward AGPAT4 over other AGPAT LPAAT family members.
CL26 binds covalently to Cys228 and noncovalently to Trp106 and Trp136 through π-π interactions.
CL26 exhibits synergistic effect of combining sorafenib in high AGPAT4-expressing MHCC97L and MHCC97H cells, the C228A mutant does not exhibit resistance to sorafenib nor show synergy with CL26.
CL26 sensitizes HCC tumors to eradication by sorafenib treatment with no evidence of toxicity in HCC PDX model.
分子量 | 306.76 | |
分子式 | C14H11ClN2O2S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Ng KY, et al. Sci Transl Med. 2025 Jul 30;17(809):eadn9472.
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