NP1867 (NP-1867)

Chemical Structure : NP1867

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货号: PC-26604Not For Human Use, Lab Use Only.

NP1867 (NP-1867) is a potent, first-in-class small molecule DNA mismatch repair (MMR) pathway modulator targeting PMS2 (PMS1 Homolog 2) with SPR KD of 65 nM for PMS2-N-terminal ATPase domain, IC50 of 22 nM in NanoBRET assays, blocks PMS2-NTD ATP binding site and inhibits DNA MMR.

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生物&药学活性

NP1867 (NP-1867) is a potent, first-in-class small molecule DNA mismatch repair (MMR) pathway modulator targeting PMS2 (PMS1 Homolog 2) with SPR KD of 65 nM for PMS2-N-terminal ATPase domain, IC50 of 22 nM in NanoBRET assays, blocks PMS2-NTD ATP binding site and inhibits DNA MMR.
NP1867 demonstrates potent and selective affinity for PMS2, with Ki of 101 nM in FP assays, covalently targets Cys73 in the PMS2-NTD.
NP1867 binds to the ATPase domain of hPMS2 through adduction of the Cys73 residue in the ATP binding site.
NP1867 shows no binding to MLH1 or Hsp90.
Co-treatment of WT-HAP1 cells with NP1867 and 6-TG resulted in dose-dependent inhibition of MMR-dependent DNA SSBs (EC50=43 nM), with maximal inhibition equivalent to PMS2 KO cells.
NP1867 also reduced the percentage of HAP1 cells undergoing 6-TG-induced and MMR-dependent cell-cycle arrest (G2/M cell population) and restored the percentage of proliferating cells in S-phase to that of cells not treated with 6-TG.
PMS2 inhibition by NP1867 leads to MSI-H status and MMR-d mutational signatures in cancer cells.
NP1867 pretreatment primes CRC tumours for anti-PD-1 response in vivo.

物理化学性质&存储条件

分子量	507.63
分子式	C29H37N3O5
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	(E)-N-(2-(2-(cyclohexylmethoxy)-4,6-dihydroxy-3-methylbenzoyl)isoindolin-4-yl)-4-(dimethylamino)but-2-enamide

参考文献

1. Blagg J, et al. Cancer Discov. 2026 Apr 21. doi: 10.1158/2159-8290.CD-26-0003.

NP1867 (NP-1867)

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NP1867 (NP-1867)

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