Product Description: CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects[1][2][3].
Applications: Cancer-Kinase/protease
Formula: C18H24Cl2N6O
References: [1]Harikumar KB, et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther. 2010 May;9(5):1136-46./[2]Xi Chen, et al. Identification and assessment of new PIM2 inhibitors for treating hematologic cancers: A combined approach of energy-based virtual screening and machine learning evaluation. Arch Pharm (Weinheim). 2024 Jan 23:e2300516./[3]Cui B, et al., Small molecule inhibitor CRT0066101 inhibits cytokine storm syndrome in a mouse model of lung injury. Int Immunopharmacol. 2023 Jul;120:110240.
CAS Number: 1883545-60-5
Molecular Weight: 411.33
Compound Purity: 99.92
Research Area: Cancer; Inflammation/Immunology
Solubility: DMSO : 11.36 mg/mL (ultrasonic;warming;heat to 60°C)/H2O : 50 mg/mL (ultrasonic)
Target: Apoptosis;Pim;PKD
English
Deutsch
