Numidargistat dihydrochloride

SKU: orb1710147

Description

Numidargistat dihydrochloride (CB-1158 dihydrochloride) is an orally bioavailable, potent arginase 1 (ARG1) inhibitor used in immuno-oncology research. It has been shown in vitro and in vivo to inhibit TGF-β2-induced cataractogenesis by suppressing lens epithelial cell proliferation and reducing markers of fibrosis like fibronectin and α-SMA.

Research Area

Immunology & Inflammation

Key Properties

• MW: 360.04
• Purity: >99.99% (May vary between batches)
• Formula: C₁₁H₂₄BCl₂N₃O₅
• SMILES: O=C([C@@H](N)C)N1C[C@H](CCCB(O)O)[C@](N)(C(O)=O)C1.Cl.Cl
• Target: Arginase
• Solubility: H2O:30 mg/mL (83.32 mM);DMSO:40 mg/mL (111.1 mM)

Bioactivity

• Target IC50:
  Arginase I:86 nM|Arginase II:296 nM
• In Vivo:
  In a mouse cancer model, Numidargistat dihydrochloride is given 100 mg/kg twice daily by oral tube feeding, and results show that Numidargistat dihydrochloride blocks arginase, The tumor growth of CT26, LLC, B16 and 4T1 was significantly inhibited.
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• In Vitro:
  Numidargistat dihydrochloride is a potent inhibitor of arginase, inhibiting recombinant human Arg1 (IC50 = 86 nM) and the related enzyme Arg2 (IC50 = 296 nM). Numidargistat dihydrochloride shows effective inhibitory activity on intracellular arginase in hepatocellular carcinoma (HCC) cell line HepG2, chronic myeloid leukemia cell line K-562, and primary human hepatocytes with IC50 of 32, 139, and 210 μM, respectively. In mouse lens culture, Numidargistat dihydrochloride (50 μM) and TGF-β2 (10 ng/ml) for 7 days indicated that ASC development could be inhibited by inhibiting ARG1.
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Storage & Handling

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

Alternative Names

INCB 01158, INCB 01158 dihydrochloride, INCB01158, INCB-01158, INCB01158 dihydrochloride, INCB-01158 Dihydrochloride, Arginase 1, Arginase 2, 2095732-06-0, 2095732-06-0 free base, CB1158, CB 1158, CB 1158 Dihydrochloride, CB 1158 dihydrochloride (2095732 06 0 free base), CB-1158, CB1158 dihydrochloride, CB-1158 dihydrochloride, CB-1158 dihydrochloride ( free base), CB1158 dihydrochloride (2095732060 free base)

Compound Identifiers

PubChem CID

137628631