CRT0066101 (trihydrochloride)

CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698) . CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056) -induced lung injury models, and has anticancer effects[1][2][3].

Product Specifications

CAS Number

[1781742-22-0]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Apoptosis; Pim; PKD

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/crt0066101-trihydrochloride.html

Smiles

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

Molecular Formula

C18H25Cl3N6O

Molecular Weight

447.79

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

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.