GSK923295 free base · Synonyms: GSK-923295 · GSK 923295

GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E kinesin motor ATPase activity.

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

Target Kinesin Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK923295 structure

CAS No.: 1088965-37-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02476-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02476-250mg	In stock	Get quote
500 mg	USD 1,530.00	BP-02476-500mg	In stock	Get quote
1 g	USD 2,450.00	BP-02476-1g	In stock	Get quote
2 g	USD 3,930.00	BP-02476-2g	In stock	Get quote
3 g	Inquire	BP-02476-3g	In stock	Inquire

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Description

GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.

Biological activity

In Vitro GSK-923295 (GSK923295) is a first-in-class, specific, allosteric inhibitor of CENP-E kinesin motor function. GSK923295 is uncompetitive with both ATP and MT, inhibiting CENP-E MT-stimulated ATPase activity with a Ki of 3.2±0.2 nM and 1.6±0.1 nM for human and canine, respectively. GSK923295 inhibits release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules[1]. GSK923295 has broad growth inhibitory activity in a panel of 237 cancer cell lines and produces significant tumor growth-delay in 8 of the 11 mouse xenograft tumor models with IC50s of 17.2 nM, 55.6 nM, 42 nM, and 51.9 nM for SW48, RKO (BRAF mutant), SW620 (KRAS mutant), and HCT116 (KRAS mutant), respectively[2]. GSK923295 is a potent and selective small molecule inhibitor of human CENPE with a Ki of 3.2 nM. GSK923295 demonstrates broad efficacy against a panel of 19 human neuroblastoma derived cell lines with an average growth IC50 of 41 nM. n Vivo Xenografts of mice treated with GSK-923295 (GSK923295) shows significant tumor growth delay compared to the control arm (NB-EBc1 p<0.0001; NB-1643 p=0.018; NB-1691 p=0.0018).

Identifiers

SMILES: CC(C)OC1=CC=C(C=C1Cl)C(=O)N[C@H](CNC(=O)CN(C)C)CC1=CC=C(C=C1)C1=CN2C=CC=C([C@H](C)O)C2=N1
InChIKey: WHMXDBPHBVLYRC-OFVILXPXSA-N

Specifications

MW (average): 592.1280
Formula: C₃₂H₃₈ClN₅O₄
CAS No.: 1088965-37-0
Physical state: Solid
Color: White to 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°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Wood KW, et al. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44.

[2]. Mayes PA, et al. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E (CENP-E) inhibition. Int J Cancer. 2013 Feb 1;132(3):E149-57.

[3]. Balamuth NJ, et al. Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target. Cancer Res. 2010 Apr 1;70(7):2749-58.

Same target

Search Kinesin

Same research area

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