KZR-616

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

KZR-616 (KZR616) 是一种有效的、选择性双免疫蛋白酶体亚基 LMP7/LMP2 抑制剂，IC50 为 39 nM/139 nM，弱抑制 β5、MECL-1，对 β1 亚基没有活性。

KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models.Other Indication Phase 2 Clinical.

Zetomipzomib also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). Zetomipzomib maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC).Zetomipzomib is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587).

Zetomipzomib (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model. Animal Model:7-8 week old female BALB/c mice (CAIA model)Dosage:I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day Administration:5 mg/kg Result:Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.

KZR616 | KZR 616

Proteasome/Ubiquitin

Proteasome

Proteasome

Other Indications

Other Disease

1629677-75-3

586.686

C30H42N4O8

>98% (HPLC)

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O=C(N[C@@H](CC1=CCCC1)C([C@]2(C)OC2)=O)[C@@H](NC([C@@H](NC(CN3CCOCC3)=O)C)=O)[C@H](O)C4=CC=C(OC)C=C4

(2S,3R)-N-((S)-3-(cyclopent-1-en-1-yl)-1-((R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide

(-20℃)

With Ice Pack

≥ 2 years