ZT-12-037-01

SKU: orb611995

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.

Research Area

Product Categories/Products/Small Molecules,Product Categories/Products/Small Molecules/Inhibitors

Key Properties

• CAS Number: [2328073-61-4]
• MW: 385.512
• Formula: C₂₁H₃₁N₅O₂
• SMILES: COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC

Storage & Handling

• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only