ZT-12-037-01

SKU: orb1225570

Description

ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 of 20.04 nM measured as percentage of NRAS phosphorylation; shows similar IC50 of 23.96 and 27.94 nM for STK19WTWT STK19D89N respectively; displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 uM; efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner, inhibits NRAS activity in a dose-dependent manner but does not affect the levels of H3K9 methylation; effectively inhibits NRAS signaling, including the MEK-ERK and PI3K pathways in SK-MEL-2 and WM2032 cells (with NRASQ61R), but the inhibition was much less effective in A375 or UACC62 cells (with NRASWT), effectively inhibits cell growth and induces apoptosis of SK-MEL-2 and WM2032 melanoma cells.

Key Properties

• CAS Number: 2328073-61-4
• MW: 385.512
• Purity: >98% (HPLC)
• Formula: C₂₁H₃₁N₅O₂
• SMILES: COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC
• Target: Ras
• Solubility: In Vitro: 1M HCl : 100 mg/mL (259.40 mM)

Bioactivity

• In Vivo:
  Animal model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes. Dosage: 25 mg/kg; 50 mg/kg. Administration: Intraperitoneally injection; 21 days; once a day. Result: Inhibited growth of SK-MEL-2 xenograft melanoma.
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• In Vitro:
  Cell Proliferation Assay Cell line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells. Concentration: 3 μM. Incubation time: 14 days. Result: Inhibited melanocyte proliferation. Western blot analysis. Cell line: STK19WT and STK19D89N. Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation time: Result: Inhibited NRAS phosphorylation.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Ras