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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-RBN012759
RBN012759

Chemical Structure : RBN012759

CAS No.: 2360851-29-0

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RBN012759 (RBN-012759)

货号: PC-49520Not For Human Use, Lab Use Only.

RBN012759 (RBN-012759) is a potent and highly selective PARP14 chemical probe inhibitor with biochemical IC50 of 3 nM in TR-FRET assays, >300-fold selectivity over all PARP family members.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg ￥8980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RBN012759 (RBN-012759) is a potent and highly selective PARP14 chemical probe inhibitor with biochemical IC50 of 3 nM in TR-FRET assays, >300-fold selectivity over all PARP family members.
RBN-012759 is an in vivo chemical probe that selectively engages PARP14 in tissue.
RBN-012759 shows binding affinity for PARP14 with Kd value of 2 nM determined by surface plasmon resonance (SPR), inhibits mouse PARP14 TR-FRET probe displacement assay with an IC50 value of 5 nM, which is comparable with its human PARP14 potency (IC50=3 nM).
RBN-012759 rubustly inhibits PARP14-specific self-MARylation in IFN-γ-stimulated primary human macrophages.
RBN-012759 reversed IL-4-driven gene expression in M2-like macrophages, including CD209, MMP-1 and CLTC. RBN-012759 also decreased the protein level of three M2-like proteins, IL-10, CCL24, and IL1-ra, in the supernatants of IL-4-stimulated macrophages.
RBN012759 induced antitumor inflammation in kidney cancer tumor explant models, elicited similar gene expression changes.

物理化学性质&存储条件

分子量 378.46
分子式 C19H23FN2O3S
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

7-(cyclopropylmethoxy)-5-fluoro-2-((((1r,4r)-4-hydroxycyclohexyl)thio)methyl)quinazolin-4(3H)-one

参考文献

1. Laurie B Schenkel , et al. Cell Chem Biol. 2021 Aug 19;28(8):1158-1168.e13.

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