MI-2

SKU: orb1227065

Description

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.

Key Properties

• CAS Number: 1047953-91-2
• MW: 455.7223
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₇Cl₃N₄O₃
• SMILES: O=C(NC1=CC=C(N2N=C(OCCOC)N=C2C3=CC=C(Cl)C(Cl)=C3)C=C1)CCl
• Target: MALT1
• Solubility: DMSO: ≥ 46 mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MI 2 | MI2

Quick Database Links

Gene Symbol

MALT1