Product Name :
CW069
Description:
CW069 is an allosteric inhibitor of HSET. CW069 showed marked activity against HSET in vitro. The inhibitor induced multipolar mitoses only in cells containing supernumerary centrosomes. CW069 therefore constitutes a valuable tool for probing HSET function and, by reducing the growth of cells containing supernumerary centrosomes, paves the way for new cancer therapeutics.
CAS:
1594094-64-0
Molecular Weight:
500.33
Formula:
C23H21IN2O3
Chemical Name:
5-Iodo-2-[[(2S)-1-oxo-3-phenyl-2-[(phenylmethyl)amino]propyl]amino]-benzoic acid
Smiles :
OC(=O)C1=CC(I)=CC=C1NC(=O)[C@H](CC1C=CC=CC=1)NCC1C=CC=CC=1
InChiKey:
IRDIXDXDSUBHIU-NRFANRHFSA-N
InChi :
InChI=1S/C23H21IN2O3/c24-18-11-12-20(19(14-18)23(28)29)26-22(27)21(13-16-7-3-1-4-8-16)25-15-17-9-5-2-6-10-17/h1-12,14,21,25H,13,15H2,(H,26,27)(H,28,29)/t21-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
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:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
CW069 is an allosteric inhibitor of HSET. CW069 showed marked activity against HSET in vitro. The inhibitor induced multipolar mitoses only in cells containing supernumerary centrosomes. CW069 therefore constitutes a valuable tool for probing HSET function and, by reducing the growth of cells containing supernumerary centrosomes, paves the way for new cancer therapeutics.|Product information|CAS Number: 1594094-64-0|Molecular Weight: 500.33|Formula: C23H21IN2O3|Synonym:|CW-069|CW 069|CW069|Chemical Name: 5-Iodo-2-[[(2S)-1-oxo-3-phenyl-2-[(phenylmethyl)amino]propyl]amino]-benzoic acid|Smiles: OC(=O)C1=CC(I)=CC=C1NC(=O)[C@H](CC1C=CC=CC=1)NCC1C=CC=CC=1|InChiKey: IRDIXDXDSUBHIU-NRFANRHFSA-N|InChi: InChI=1S/C23H21IN2O3/c24-18-11-12-20(19(14-18)23(28)29)26-22(27)21(13-16-7-3-1-4-8-16)25-15-17-9-5-2-6-10-17/h1-12,14,21,25H,13,15H2,(H,26,27)(H,28,29)/t21-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|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.{{Relacorilant} site|{Relacorilant} Vitamin D Related/Nuclear Receptor|{Relacorilant} Technical Information|{Relacorilant} Formula|{Relacorilant} supplier|{Relacorilant} Autophagy} |Shelf Life: ≥12 months if stored properly.{{Calcein} web|{Calcein} {Fluorescent Dye}|{Calcein} Purity & Documentation|{Calcein} References|{Calcein} manufacturer|{Calcein} Epigenetic Reader Domain} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:23746961 |Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM. CW-069 shows statistically significant selectivity over KSP. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC50 of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells.|References:|Watts CA, Richards FM, Bender A, Bond PJ, Korb O, Kern O, Riddick M, Owen P, Myers RM, Raff J, Gergely F, Jodrell DI, Ley SV. Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes. Chem Biol. 2013 Nov 21;20(11):1399-410. doi: 10.1016/j.chembiol.2013.09.012. PubMed PMID: 24210220; PubMed Central PMCID: PMC3898838.Bhakta-Guha D, Saeed ME, Greten HJ, Efferth T. Dis-organizing centrosomal clusters: specific cancer therapy for a generic spread? Curr Med Chem. 2015;22(6):685-94. Review. PubMed PMID: 25515519.Products are for research use only. Not for human use.|