KGP94

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

KGP94 是一种有效的、选择性的、竞争性的溶酶体内肽酶抑制剂。

KGP94 is a potent, selective, and competitive inhibitor of the lysosomal endopeptidase enzyme.(In Vitro):The novel cathepsin L/K inhibitors KGP94 could inhibit in vitro M2 macrophage invasion and reduce the macrophage-stimulated invasion of 4T1 murine breast cancer cells. KGP94 treatment also reduced the expression of several M2-associated markers, suggesting that cathepsin L activity may be important for IL-4-driven M0 to M2 differentiation.

KGP94 (10 or 20 μM, 24 h) reduces expression of M2 (macrophage) markers (Arginase-1 and CD206) and cells invasion of primary bone marrow-derived macrophages or Raw264.7.KGP94 (25 μM, 24 h) impairs the incasive capacities of both prostate and breat cancer cells by 53% and 88%, respectively.KGP94 (25 μM, 24 h) suppresses secreted CTSL activity by 94% and 92% in PC-3ML and MDA-MB-231, repsectively. Cell Invasion Assay Cell Line:PC-3ML, MDA-MB-231 Concentration:10 μM, 25 μM Incubation Time:24 hours Result:Attenuated migration and invasion of prostate and breast cancer cells.

KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model. Animal Model:NCR nu/nu male mice Dosage:20 mg/kg Administration: Intraperitoneal injection; once daily for 3 days Result:Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.

KGP 94 | KGP-94

Proteasome/Ubiquitin

Cysteine Protease

Antibacterial

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1131456-28-4

350.23

C14H12BrN3OS

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (285.53 mM)

NC(=S)N\N=C(/c1cccc(O)c1)c1cccc(Br)c1

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(-20℃)

With Ice Pack

≥ 2 years