K-Ras-PDEδ-IN-1

• CAT Number: I030154
• CAS Number: 1841464-21-8
• Molecular Formula: C25H26FN5O2
• Molecular Weight: 447.5144
• Purity: 98%
• Synonyms: K-Ras-PDEδ-IN-1
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: N-(4-fluorophenethyl)-4-(4-methyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide
• InChI: InChI=1S/C25H26FN5O2/c1-17-5-11-21(12-6-17)31-16-22-18(2)28-30(25(33)24(22)29-31)15-3-4-23(32)27-14-13-19-7-9-20(26)10-8-19/h5-12,16H,3-4,13-15H2,1-2H3,(H,27,32)
• InChIKey: RRELLHHWESTKAK-UHFFFAOYSA-N
• SMILES: O=C(NCCC1=CC=C(F)C=C1)CCCN2N=C(C)C3=CN(C4=CC=C(C)C=C4)N=C3C2=O

K-Ras-PDEδ-IN-1(cat: I030154) is a novel and potent competitive inhibitor of K-Ras-PDEδ. It specifically targets the farnesyl binding pocket of PDEδ. K-Ras is an important oncogenic protein involved in various cancers, and inhibiting its activity has therapeutic potential. PDEδ plays a crucial role in the farnesylation process of K-Ras, and by binding to its farnesyl binding pocket, K-Ras-PDEδ-IN-1 disrupts this process, inhibiting the activation of K-Ras. This inhibition can potentially hinder the growth and proliferation of cancer cells driven by aberrant K-Ras signaling.

Reference

1: Murarka S, Martín-Gago P, Schultz-Fademrecht C, et al. Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site. Chemistry. 2017;23(25):6083-6093. doi:10.1002/chem.201603222