CRT0066101 dihydrochloride salt form · dihydrochloride · Parent CRT-0066101

CRT0066101 is a potent inhibitor of protein kinase D.

For research use only. Not for human or veterinary use.

Target PKD Pim Apoptosis

Research area Inflammation/Immunology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CRT0066101 dihydrochloride structure

CAS No.: 1883545-60-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 460.00	BP-02133A-50mg	In stock	Get quote
100 mg	USD 720.00	BP-02133A-100mg	In stock	Get quote
200 mg	USD 1,120.00	BP-02133A-200mg	In stock	Get quote
500 mg	USD 2,280.00	BP-02133A-500mg	In stock	Get quote
1 g	USD 3,650.00	BP-02133A-1g	In stock	Get quote

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Description

CRT0066101 is a potent inhibitor of protein kinase D (PKD). CRT0066101 inhibits all PKD isoforms.

Biological activity

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. 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. 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. 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.

Identifiers

SMILES: Cl.Cl.CC[C@@H](N)CNC1=NC(=NC=C1)C1=C(O)C=CC(=C1)C1=CN(C)N=C1
InChIKey: CXYCRYGNFKDPRH-FMOMHUKBSA-N

Specifications

MW (average): 411.3290
Formula: C₁₈H₂₄Cl₂N₆O
CAS No.: 1883545-60-5
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

Same target

Search PKD

Same research area

Search Inflammation/Immunology