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CID 2011756

Catalog No.
A8223
PKD inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$69.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$60.00
In stock
10mg
$95.00
In stock
50mg
$410.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

CID-2011756 is a novel and potent inhibitor of protein kinase D1 (PKD1), one of three PKD isoforms of a novel family of serine/threonine kinases involved in cell proliferation, survival, invasion and protein transport, with a value of 50% inhibition concentration IC50 of 3.2 μM in vitro. CID-2011756 also exhibits pan-PKD inhibitory effects that ATP-competitively inhibits PKD2 and PDK3 with values of IC50 of 0.6 μM and 0.7 μM respectively. Study results have shown that CID-2011756 is a cell active PKD1 inhibitor that concentration-dependently inhibits phorbolester-induced endogenous PKD1 activation in LNCap prostate cancer cells with a value of half maximal effective concentration EC50 of 10 μM.

Reference

Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.

Chemical Properties

Physical AppearanceA solid
StorageStore at RT
M.Wt396.87
Cas No.638156-11-3
FormulaC22H21ClN2O3
Solubility≥39.7 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥2.34 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name5-(3-chlorophenyl)-N-[4-(morpholin-4-ylmethyl)phenyl]furan-2-carboxamide
SDFDownload SDF
Canonical SMILESC1COCCN1CC2=CC=C(C=C2)NC(=O)C3=CC=C(O3)C4=CC(=CC=C4)Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description CID-2011756 is a cell-active ATP competitive and specific inhibitor of PKD1.
Targets PKD          
IC50 10±0.7 μM          

Quality Control

Chemical structure

CID 2011756

Related Biological Data

CID 2011756