NI-57

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NI-57 是 BRPF 溴结构域的有效抑制剂，可与 BRPF1B、BRPF2 和 BRPF3 结合，KD 分别为 31 nM、108 nM 和 408 nM (ITC)。

NI-57 is a potent inhibitor of the bromodomain of the BRPFs and binds to BRPF1B, BRPF2 and BRPF3 and with KD of 31 nM,108 nM and 408 nM (ITC), respectively; shows highly selectivity against other non-Class IV bromodomains, including the BETs, as measured by both biophysical and biochemical methods; displays 32-fold selectivity over the closest off-target BRD9; shows accelerated FRAP recovery at 1 uM in the BRPF2 FRAP assay preventing binding of full-length BRPF2 to chromatin.

NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2 nM, BRD1 with a Kd of 110 ± 13 nM, and BRPF3 with a Kd of 410 ± 47 nM, whereas binding to BRD9 is weaker (Kd 1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%.

NI-57 has favorable oral bioavailability in mice.

BRPF inhibitor NI57

Chromatin/Epigenetic

Bromodomain

Bromodomain

Cancer

——

1883548-89-7

383.422

C19H17N3O4S

>98% (HPLC)

DMSO : ≥ 83.3 mg/mL 217.26 mM

O=S(C1=CC=C(C#N)C=C1OC)(NC2=CC3=C(N(C)C(C(C)=C3)=O)C=C2)=O

4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years