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MedChemExpress - Model CRT0066101 ...

MedChemExpress - Model CRT0066101 dihydrochloride - 1883545-60-5

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].

CRT0066101 dihydrochloride

MCE China：CRT0066101 dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-15698A

CAS：1883545-60-5

Purity：99.92%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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. 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.

In Vitro：CRT0066101 (5 µM; 1 h) dihydrochloride blockS both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 dihydrochloride abrogates NT-induced phosphorylation of Hsp27 (pS82-Hsp27), attenuates PKD1-mediated NF-κB activation, and abrogates expression of NF-κB-dependent-dependent proliferative and pro-survival proteins[1]. CRT0066101 dihydrochloride significantly inhibits Panc-1 cell proliferation, with an IC50 value of 1 µM. CRT0066101 dihydrochloride results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 dihydrochloride significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but had a modest effect in Capan-2 cells[1].

In Vivo：CRT0066101 dihydrochloride (80 mg/kg/day; oral gavage; once daily; for 21 days) dihydrochloride in Panc-1 orthotopic model potently blocks tumor growth in vivo[1]. CRT0066101 dihydrochloride (10 mg/kg, i.p., every two days for 3 times) exhibits a protective effect against LPS-induced pneumonia and alleviates lung damage in C57BL/6J mice[3].

IC50 & Target：PKD1 1 nM (IC50) PKD3 2 nM (IC50) PKD2 2.5 nM (IC50) PIM2 135.7 nM (IC50)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。