CRT0066101

CRT0066101 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 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056) -induced lung injury models, and has anticancer effects[1][2][3].

Product Specifications

CAS Number

[956123-34-5]

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

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.html

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

N[C@H](CC)CNC1=NC(C2=C(O)C=CC(C3=CN(C)N=C3)=C2)=NC=C1

Molecular Formula

C18H22N6O

Molecular Weight

338.41

Precautions

H302, H312, H332

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.