MS2928 TFA | SETD8 inhibitor | Probechem Biochemicals

Chemical Structure : MS2928 TFA

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MS2928 TFA (MS-2928 TFA)

货号: PC-28194Not For Human Use, Lab Use Only.

MS2928 TFA is a potent and selective SETD8 covalent inhibitor, inhibits SETD8 methyltransferase activity with IC50 of 0.14 uM, covalently modifies SETD8 at Cys311.

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生物&药学活性

MS2928 TFA is a potent and selective SETD8 covalent inhibitor, inhibits SETD8 methyltransferase activity with IC50 of 0.14 uM, covalently modifies SETD8 at Cys311.
MS2928 displays excellent selectivity for SETD8 over 20 other methyltransferases.
MS2928 shows potent cellular activity, effectively reducing H4K20me1 levels and inhibiting cancer cell proliferation in SETD8-overexpressing MM cell lines, while sparing SETD8-low expressing MM cells and normal cells.
MS2928 induces significant growth inhibition of both JJN-3 and OPM-2 cells in a concentration-dependent manner, with IC50 values of 1.06 ± 0.13 and 0.54 ± 0.05 μM, respectively.
MS2928 (25 mg/kg, i.p.) effectively suppressed tumor growth in vivo in SETD8-overexpressing MM cell line xenograft mouse models.

物理化学性质&存储条件

分子量	526.51
分子式	C23H29F3N6O5
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	2-Propynamide, N-[3-[[7-(2-aminoethoxy)-6-methoxy-2-(1-pyrrolidinyl)-4-quinazolinyl]amino]propyl]-, 2,2,2-trifluoroacetate (1:1)

参考文献

1. He Chen, et al. J Med Chem. 2026 Feb 26;69(4):4255-4269.

MS2928 TFA (MS-2928 TFA)

生物&药学活性

物理化学性质&存储条件

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MS2928 TFA (MS-2928 TFA)

生物&药学活性

物理化学性质&存储条件

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