CRT0066101 (dihydrochloride)
Product Specifications
UNSPSC 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].
Target Antigen
Apoptosis; Pim; PKD
Type
Reference compound
Related Pathways
Apoptosis;JAK/STAT Signaling
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/CRT0066101_dihydrochloride.html
Solubility
DMSO : 11.36 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : 50 mg/mL (ultrasonic)
Smiles
OC1=CC=C(C2=CN(C)N=C2)C=C1C3=NC=CC(NC[C@H](N)CC)=N3.[H]Cl.[H]Cl
Molecular Weight
411.33
References & Citations
[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.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-15698A/CRT0066101-dihydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-15698A/CRT0066101-dihydrochloride-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
1883545-60-5
Available Sizes
Curated Selection
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