1. Metabolic Enzyme/Protease
    NF-κB
  2. MALT1
  3. MLT-231

MLT-231 

Cat. No.: HY-131902
Handling Instructions

MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.

For research use only. We do not sell to patients.

MLT-231 Chemical Structure

MLT-231 Chemical Structure

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Description

MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse[1].

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: OCI-Ly3 cells
Concentration: 50-5000 nM
Incubation Time: 24 hours
Result: NF-κB target gene IRF4 was 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[1].
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[1].
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[1].
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[1].
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)[1]
Dosage: 10, 30, and 100 mg/kg
Administration: P.o.; bid schedule for 2 weeks
Result: Led to tumor stasis, while being well tolerated.
Molecular Weight

469.85

Formula

C₁₉H₁₉ClF₃N₇O₂

SMILES

O=C(NC1=C(N2[[email protected]@H](C)COC[[email protected]@H]2C)N3C(N=C1)=CC(Cl)=N3)NC4=CC=NC(C(F)(F)F)=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MLT-231MLT231MLT 231MALT1mucosa associated lymphoid tissue lymphoma translocation gene 1primaryimmunecellsBlymphomaantitumorABC-DLBCLtypexenograftmodelInhibitorinhibitorinhibit

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MLT-231
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HY-131902
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