CZC24832

SKU: orb1307007

Description

CZC24832

Research Area

Signal Transduction

Key Properties

• CAS Number: 1159824-67-5
• MW: 364.4
• Purity: 99.08% (May vary between batches)
• Formula: C₁₅H₁₇FN₆O₂S
• SMILES: CC(C)(C)NS(=O)(=O)c1cncc(c1)-c1cc(F)c2nc(N)nn2c1
• Target: PI3K
• Solubility: DMSO:36.4 mg/mL (99.89 mM);10% DMSO+90% Corn Oil:2 mg/mL (5.49 mM)

Bioactivity

• Target IC50:
  PI3Kβ:1.1 μM|PI3Kγ:27 nM|PI3Kδ:8.194 μM
• In Vivo:
  In the BT system, treatment with CZC24832 significantly inhibits IL-17A (IC50 = 1.5 μM) as well as B-cell activation markers, such as IL-6 and IgG. Moreover, in T-cell systems, such as in human umbilical vein endothelial cells, the production of IL17A is strongly suppressed, indicating that PI3Kγ kinase activity plays a broad role in the functionality of TH17 cells. Accordingly, CZC24832 inhibits the differentiation of TH17 cells. A high-throughput screening of 154 lipid and protein kinases, alongside 922 other proteins, identified only PI3Kβ and PIP4K2C as off-target proteins within a 100-fold selectivity window.
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• In Vitro:
  In a therapeutic model of collagen-induced arthritis (CIA), mice administered 10 mg/kg of CZC24832 orally twice daily exhibited significant reductions in both bone and cartilage destruction and overall clinical parameters. Additionally, in an IL-8-dependent air-pouch model, CZC24832 demonstrated a dose-dependent decrease in granulocyte recruitment, consistent with the level of inhibition observed in mice lacking PI3Kγ.
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Storage & Handling

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

Alternative Names

inhibit, Inhibitor, CZC 24832, CZC24832, CZC-24832, PI3K, PI3Kδ, PI3Kβ, PI3Kγ, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

42623951