1. Metabolic Enzyme/Protease
    NF-κB
  2. MALT1
  3. MLT-943

MLT-943 

Cat. No.: HY-134820
Handling Instructions

MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.

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

MLT-943 Chemical Structure

MLT-943 Chemical Structure

CAS No. : 1832576-04-1

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research[1].

In Vitro

MLT-943 shows a high potency and selectivity in vitro. MLT-943 inhibits stimulated IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood)[1].

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

In Vivo

MLT-943 (oral gavage; 10 mg/kg; QD) prophylactic treatment in the rat collagen-induced arthritis model suppresses anti-collagen antibody production, fully prevents paw swelling, and normalizes joint histology scores in rat model[1].
MLT-943 (oral gavage; 5 mg/kg; QD; 10 consecutive days) effectively inhibits MALT1 protease activity and results in a progressive reduction in the frequency of Foxp3+CD25+ Treg cells in circulating CD4+ T cells, which was maximal after 7 days of treatment. And Discontinuation of MLT-943 treatment after day 10 leads to Treg frequency progressively returning to their original values within 4 days. Suboptimal doses of MLT-943 (0.1 and 0.5 mg/kg QD; p.o.) does not impact the Treg frequency[1].
MLT-943 (oral gavage; 0, 5, 20 or 80 mg/kg/day; 4-13 weeks) causes a reduction in Treg and an increase in total T cell counts, in both 4- and 13-week rat toxicity studies at all dose levels. While a 4-Longer treatment induces severe immune-mediated pathology in multiple organs, with clinical onset starting around week 9 in rat[1].
MLT-943 (p.o. admistration; 3 mg/kg; single dose) exhibits a good PK parameters in vivo. The Cmax values are 0.7 nM and 0.5 nM, respectively in rat and mice, respectively. And the F% are 86% and 50% in rat and mice, respective[1].
For i.v. admistration the compound is formed in NMP:PEG200 (30/70); For p.o. admistration solution is formed in MC:Tween 80:Water (0.5:0.5:99) solution (Sourced from literature, for reference only)[1].

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

Animal Model: Naïve rats[1]
Dosage: 5 mg/kg
Administration: Oral gavage; 5 mg/kg, 10 consecutive days or 0.1 mg/kg MLT-943
Result: Induced a severe immune-mediated pathology after a prolonged treatment
Molecular Weight

414.77

Formula

C₁₆H₁₄ClF₃N₆O₂

CAS No.
SMILES

CO[[email protected]](C1=C(NC(NC2=CC=NC(C(F)(F)F)=C2)=O)C=NC3=CC(Cl)=NN13)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MLT-943MLT943MLT 943MALT1mucosa associated lymphoid tissue lymphoma translocation gene 1anti-inflammatoryinflammationpaw swellingInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MLT-943
Cat. No.:
HY-134820
Quantity:
MCE Japan Authorized Agent: