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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-KMR-206
KMR-206

Chemical Structure : KMR-206

CAS No.: 2992741-10-1

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KMR-206 (KMR206)

货号: PC-49585Not For Human Use, Lab Use Only.

KMR-206 (KMR206) is a potent, selective PARP7 inhibitor with IC50 of 13.7 nM, displays 75-fold selectivity for PARP7 over PARP2 and does not inhibit PARP1 up to 3 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    KMR-206 (KMR206) is a potent, selective PARP7 inhibitor with IC50 of 13.7 nM, displays 75-fold selectivity for PARP7 over PARP2 and does not inhibit PARP1 up to 3 uM.
    KMR-206 is more than 50-fold selective for PARP7 over most PARP family members beyond PARP1 and PARP2, KMR-206 still exhibits an approximately 10-fold selectivity for PARP7 over MARylating PARPs (PARP10 and PARP11).
    KMR-206 dose-dependently decreases PARP7 MARylation in GFP-PARP7-expressing HEK 293T cells with EC50 of 8 nM.
    KMR-206 (100 nM) inhibits PARP7 catalytic activity and derepresses AHR ligand-mediated gene transcription in MEFs, stimulates IFN-β transcription and acts synergistically with 3pRNA and cGAMP.
    KMR-206 (0.01-0.3 uM) increase STAT1 and phospho-Tyr701-STAT1 (pSTAT1) in a dose-dependent manner, induces an STING-dependent type I IFN response and PARP7 protein accumulation in CT-26 cells.
    KMR-206 dose-dependently decreases the viability of NCI-H1373 cells with EC50 of 104 nM, increases PARP7 abundance in the nucleus in HiBiT-PARP7 knockin (KI) CT-26 cells.

    物理化学性质&存储条件

    分子量 506.541
    分子式 C29H23FN6O2
    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

    6-(4-(2-fluoro-5-((4-oxo-7-(prop-1-yn-1-yl)-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)nicotinonitrile

    参考文献

    1. Daniel J Sanderson, et al. Cell Chem Biol. 2022 Dec 16;S2451-9456(22)00418-4.

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