ZCL278, Cdc42 GTPase Inhibitor


Catalog No. size PriceQuantity
M60133-2S 2mg solid $119
M60133-10S 10mg solid $482
M60133-100 100mg solid $1,710
M60133-100S 100mg solid $1,710

Description

ZCL278 is a potent and selective inhibitor of Cdc42 GTPase. ZCL278 directly binds to the binding site of the Cdc42 guanine nucleotide exchange factor intersectin (ITSN) and inhibits its functions (Kd ~6-11 µM). In Swiss 3T3 fibroblast cultures, ZCL278 abolished microspike formation and disrupted GM130-docked Golgi structures, two of the most prominent Cdc42-mediated subcellular events. ZCL278 reduces the perinuclear accumulation of active Cdc42 in contrast to NSC23766, a selective Rac inhibitor. ZCL278 suppresses Cdc42-mediated neuronal branching and growth cone dynamics as well as actin-based motility and migration in a metastatic prostate cancer cell line (i.e., PC-3) without disrupting cell viability. ZCL278 could be a powerful chemical tool for research of Cdc42 subclass of Rho GTPases in human pathogenesis, such as those of cancer and neurological disorders.

Product information

CAS Number: 587841-73-4

Molecular Weight: 584.89

Formula: C21H19BrClN5O4S2

Chemical Name: 2-(4-bromo-2-chlorophenoxy)-N-((4-(N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl)phenyl)carbamothioyl)acetamide

Smiles: CC1C=C(C)N=C(NS(=O)(=O)C2C=CC(=CC=2)NC(=S)NC(=O)COC2=CC=C(Br)C=C2Cl)N=1

InChiKey: XKZDWYDHEBCGCG-UHFFFAOYSA-N

InChi: InChI=1S/C21H19BrClN5O4S2/c1-12-9-13(2)25-20(24-12)28-34(30,31)16-6-4-15(5-7-16)26-21(33)27-19(29)11-32-18-8-3-14(22)10-17(18)23/h3-10H,11H2,1-2H3,(H,24,25,28)(H2,26,27,29,33)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ZCL278 was used at 50 µM final concentration in various in vitro assays.

References:

  1. Friesland A, et al. Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. (2013) Proc Natl Acad Sci USA. 110(4):1261-6.

Products are for research use only. Not for human use.

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