Y320

SKU: orb1225422

Description

Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.

Key Properties

• CAS Number: 288250-47-5
• MW: 505.01
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₉ClN₆O₂
• SMILES: O=C(C1=C(C)N(C2=CC=C(Cl)C=C2)N=C1)NC3=CC=C(N4CCC(N5CCOCC5)CC4)C(C#N)=C3
• Target: Lipase
• Solubility: DMSO: 11 mg/mL (21.78 mM)

Bioactivity

• In Vivo:
  Y-320 (0-3 mg/kg; p.o. ; daily, for 42 d) ameliorates collagen-induced arthritis (CIA) in DBA/1J mice with a reduction of IL-17 mRNA in arthritic joints. Y-320 (5 mg/kg; i. v. ; every three days, for 18 d; Homozygous nude athymic mice with Bats-72 xenograft) sensitizes MDR xenograft tumor to Paclitaxel In vivo. Animal model: Type II collagen-induced arthritis (CIA) in DBA/1J mice. Dosage: 0, 0.1, 0.3, 1, and 3 mg/kg. Administration: Oral administration; daily, for 42 days. Result: Inhibited the development of CIA and the increase in paw thickness in a dose-dependent manner. Inhibited joint destructions in a dose-dependent manner. Improved inflammation and damage in the arthritic ankle joints in CIA mice. Animal model: Homozygous nude athymic mice with Bats-72 xenograft (female, 4-5 weeks old). Dosage: 5 mg/kg; Paclitaxel (5 mg/kg). Administration: Intravenous injection; every three days, for 18 days. Result: Inhibited tumor growth in Bats-72 xenografts without severe adverse effects.
• In Vitro:
  Y-320 (0-100 nM; 48 h) inhibits IL-17 production by murine and human CD4 T Cells stimulated with IL-15 with IC50 values of 25.7, 52.4 and 57.4 nM for murine CD4 T cells, murine Th17 cells and human CD4 T cells, respectively. Y-320 (0-100 nM; 48 h) inhibits phosphorylation of JAK1/JAK3 in murine CD4 T cells stimulated with IL-15/CXCL12/anti-CD3 mAb. Y-320 (0.25-2 μM; 48 h) enhances PTC readthrough by G418 in different cell lines. Y-320 (0-2 μM; 48 h; HDQ-P1 cells) increases cellular protein levels and ribosome biogenesis in a concentration-dependent manner. Y-320 (0-2 μM; 48 h; Tsc2-/- cells) causes a small decrease in phospho-S6K combination with G418 (100 μM). Y-320 (1 μM; 48 h; HDQ-P1 cells) up-regulates CXC chemokine expression including CXCL10, CXCL8, and CXCL2.Y-320 (500 nM; 72 h) reverses the resistance to paclitaxel in MDR cancer cells. Y-320 has the reversal index (RI) combined with Paclitaxel (0-1000 nM) are 5.5 (Bads-200), 9.4 (Bats-72) and 1.7 (Huh7-TS-48). Y-320 (500 nM; 72 h; Bads-200 cells) enhances Paclitaxel-induced G2/M arrest and enhances Paclitaxel-induced (500 nM) tumor cell apoptosis. Y-320 (0-20 μM; 72 h; Bads-200 cells) is a substrate of P-gp reverses MDR by inhibiting P-gp function. Cell Cycle Analysis Cell line: Bads-200 cells. Concentration: 500 nM. Incubation time: 72 hours. Result: Increased the percentage of cells at G2/M phase, from 6.3% to 42.5%. Apoptosis Analysis Cell line: Bads-200 cells. Concentration: 500 nM. Incubation time: 72 hours. Result: Increased the ratio of apoptotic Bads-200 cells (30.8% versus 2.2%).

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

Y-320 | Y320 | Y 320

Quick Database Links

Gene Symbol

Lipase