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MCE 国际站:MLT-231
产品活性:MLT-231 是一种高效、高选择性的变构 MALT1 抑制剂,IC50 为 9 nM。MLT-231 特异性地阻止内源性 BCL10 断裂,IC50 为 160 nM。MLT-23 在 ABC-DLBCL 型异种移植模型中具有抗肿瘤活性。
研究领域:Metabolic Enzyme/Protease | NF-κB
作用靶点:MALT1
In Vitro: MLT-231 (19.5-10000 nM) inhibits the proliferation of OCI-Ly3 cells. MLT-231 (50-5000 nM; 24 hours) leads to accumulation of the uncleaved form of its substrates CYLD, BCL10, and RELB while expression of the NF-κB target gene IRF4 is suppressed.
In Vivo: MLT-231 (10-100 mg/kg; p.o.; bid schedule for 2 weeks) displays in vivo efficacy in the ABC-DLBCL xenograft model.
MLT-231 (1 mg/kg; i.v.; BALB/c mice) treatment shows the CL, t1/2, and Vss are 11 mL/min/kg, 1.9 hours, and 1.5 L/kg, respectively.
MLT-231 (1 mg/kg; i.v.; Sprague-Dawley rats) treatment shows the CL, t1/2, and Vss are 41 mL/min/kg, 3.2 hours, and 9.4 L/kg, respectively.
MLT-231 (3 mg/kg; p.o.; BALB/c mice) treatment shows the AUC0-24, Cmax and F are 3096 nM/h, 549 nM, and 99%, respectively.
MLT-231 (3 mg/kg; p.o.; Sprague-Dawley rats) treatment shows the AUC0-24, Cmax and F are 547 nM/h, 46 nM, and 61%, respectively.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Metabolism/Protease Compound Library | NF-κB Signaling Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | Highly Selective Inhibitors Library | MALT1-IN-3 | MLT-943 | Mepazine hydrochloride | MALT1-IN-5 | MALT1-IN-6 | MALT1-IN-7 | MLT-747 | RGT-068A | MLT-748 | MALT1-IN-9 | NVS-MALT1 | (R)-MLT-985 | MALT1 inhibitor MI-2 | Z-VRPR-FMK TFA | Val-Arg-Pro-DL-Arg-Fluoromethylketone | MALT1-IN-8 | MALT1-IN-11 | Safimaltib
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货号: HY-131902
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