MI-2

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

MI-2（MALT1 抑制剂）是一种选择性、不可逆的 MALT1 副半胱天冬酶抑制剂，IC50 为 5.84 uM。

MI-2 (MALT1 inhibitor) is a selective, irreversible MALT1 paracaspase inhibitor with IC50 of 5.84 uM, displays little activity against the related caspase family members caspase-3, -8, and -9; inhibits cleavage of MALT1 substrates, which is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation; specifically suppress ABC-DLBCL in vitro and in vivo, exhibits GI 50 of 0.2, 0.5, 0.4, and 0.4 uM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells respectively, inhibits nuclear translocation of RelB and p50, and decreases Bcl-xL levels in CLL cells.

MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 μM, respectively.MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage. Cell Proliferation Assay Cell Line:HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells Concentration:1, 10, 100, 1000 nM Incubation Time:48 hours Result:The GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 μM, respectively.Western Blot Analysis Cell Line:HBL-1 cells Concentration:62, 125, 250, 500, 1000 nM Incubation Time:24 hours Result:Inhibits MALT1 cleavage of CYLD in HBL-1 cells.

MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts. Animal Model:Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells) Dosage:25 mg/kg Administration:Intraperitoneal injection; daily for 14 days Result:Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle.

MI 2 | MI2

NF-κB

MALT1

MALT1

Inflammation/Immunology

——

1047953-91-2

455.7223

C19H17Cl3N4O3

>98% (HPLC)

DMSO: ≥ 46 mg/mL

O=C(NC1=CC=C(N2N=C(OCCOC)N=C2C3=CC=C(Cl)C(Cl)=C3)C=C1)CCl

Acetamide, 2-chloro-N-[4-[5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years