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CCT251545

Catalog No. T14907 CAS 1661839-45-7

CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).

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CCT251545, CAS 1661839-45-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 57.00
5 mg	In stock	$ 90.00
10 mg	In stock	$ 157.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 571.00
100 mg	In stock	$ 819.00
1 mL * 10 mM (in DMSO)	In stock	$ 90.00

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Purity: 99.37%

Purity: 98.2%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).
Targets&IC50	WNT (7dF3 cells):5 nM
In vitro	CCT251545, a small-molecule inhibitor of the WNT pathway discovered through cell-based screening, is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.?X-ray crystallography demonstrates a type 1 binding mode involving insertion of the CDK8 C terminus into the ligand binding site.?In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity.?We show that CCT251545 and close analogs alter WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.?Consistent with this, we find that phosphorylation of STAT1(SER727) is a biomarker of CDK8 kinase activity in vitro and in vivo[1].
In vivo	In vivo, CCT251545 with WNT-dependent tumors activity[1].

Molecular Weight	421.92
Formula	C23H24ClN5O
CAS No.	1661839-45-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45mg/ml (106.66 Mm)

References and Literature

1. Dale T, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-980. 2. Mallinger A, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem. 2015 Feb 26;58(4):1717-35.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Compound Library Osteogenesis Compound Library Bioactive Compounds Library Max Reprogramming Compound Library Wnt/Hedgehog/Notch Compound Library Anti-Fibrosis Compound Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Lung Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CCT251545 1661839-45-7 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin inhibit Wnt Inhibitor CCT 251545 CCT-251545 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.