GSK484 hydrochloride

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

GSK484 盐酸盐 (GTPL8577) 是一种特异性、可逆的肽基精氨酸脱亚胺酶 4 (PAD4) 抑制剂。

GSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor. It demonstrates high-affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.GSK484 demonstrates high-affinity binding to the low-calcium form of PAD4 with IC50s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner.To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppresses the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity.

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GTPL8577,AOB6992

Others

Other Targets

PAD4

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1652591-81-5

510.03

C27H30ClN5O3

>98% (HPLC)

DMSO:60 mg/mL (117.64 mM; Need ultrasonic)

Cl.COC1=CC(=CC2=C1N(C)C(=N2)C1=CC2=CC=CC=C2N1CC1CC1)C(=O)N1CC[C@@H](O)[C@@H](N)C1

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(-20℃)

With Ice Pack

≥ 2 years