JKE-1674

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

JKE-1674 是谷胱甘肽过氧化物酶 4 (GPX4) 的抑制剂。 JKE-1674 是 GPX4 抑制剂 ML-210 的活性代谢物。

JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4). JKE-1674 is an active metabolite of the GPX4 inhibitor ML-210.(In Vitro):JKE-1674 reduces the viability of LOX-IMVI cancer cells with an EC50 of 0.03 μM and in a panel of additional cancer cell lines. JKE-1674 is completely rescued by ferroptosis inhibitors.(In Vivo):JKE-1674 (50?mg/kg; p.o.) could be detected in the serum of mice dosed orally with the compound.

JKE-1674 exhibits activity indistinguishable from that of ML210 in cellular target engagement assays including yielding the same +434Da GPX4 adduct in cells. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors. JKE-1674 forms a nitrile-oxide electrophile in cells. JKE-1674 dehydration yields a nitrile-oxide electrophile that binds GPX4. JKE-1674 exhibits far greater stability than chloroacetamide inhibitors.

JKE-1674 (50?mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound. Animal Model:SCID mice Dosage:50?mg/kg (Pharmacokinetic Analysis)Administration:P.o.Result:Could be detected in the serum of mice dosed orally with the compound.

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Others

Other Targets

IL-5

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2421119-60-8

451.3

C20H20Cl2N4O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (221.58 mM)

O=C(C(C[N+]([O-])=O)=NO)N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1

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(-20℃)

With Ice Pack

≥ 2 years