Art. -Nr.: HY-10299

GSK-923295

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

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Reinheit: 99.95%
CAS. Nr.: 1088965-37-0
Formel: C₃₂H₃₈ClN₅O₄
Molecular Weight:592.13

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK-923295 Chemical Structure

CAS. Nr.: 1088965-37-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (41)
Lösungsmittel & Löslichkeit
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- In Vivo
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CENP-E

1.6 nM (Ki, Canine CENP-E)

Alle Kinesin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
5637	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human 5637 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human 5637 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
639-V	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human 639-V cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human 639-V cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
647-V	GI₅₀	72 nM Compound: GSK923295	Anticancer activity against human 647-V cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human 647-V cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
786-0	GI₅₀	45 nM Compound: GSK923295	Anticancer activity against human 786-0 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human 786-0 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A 172	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human A-172 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A-172 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A101D	GI₅₀	17 nM Compound: GSK923295	Anticancer activity against human A101D cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A101D cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A204	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human A204 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A204 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A2780	GI₅₀	13 nM Compound: GSK923295	Anticancer activity against human A2780 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A2780 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A-375	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human A-375 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A-375 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A-427	GI₅₀	97 nM Compound: GSK923295	Anticancer activity against human A-427 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A-427 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A-431	GI₅₀	21 nM Compound: GSK923295	Anticancer activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A498	GI₅₀	81 nM Compound: GSK923295	Anticancer activity against human A498 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A498 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A549	GI₅₀	21 nM Compound: GSK923295	Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
A673	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human A673 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human A673 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
ACHN	GI₅₀	61 nM Compound: GSK923295	Anticancer activity against human ACHN cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human ACHN cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
AGS	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human AGS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human AGS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
AN3-CA	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human AN3-CA cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human AN3-CA cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
ARH-77	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human ARH-77 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human ARH-77 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BC-3	GI₅₀	88 nM Compound: GSK923295	Anticancer activity against human BC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BE(2)-C	GI₅₀	93 nM Compound: GSK923295	Anticancer activity against human BE2C cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BE2C cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BeWo	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human BeWo cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BeWo cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BFTC-905	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human BFTC-905 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BFTC-905 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BHT-101	GI₅₀	100 nM Compound: GSK923295	Anticancer activity against human BHT-101 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BHT-101 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BPH-1	GI₅₀	52 nM Compound: GSK923295	Anticancer activity against human BPH-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BPH-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BT-20	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human BT-20 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BT-20 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BT-474	GI₅₀	110 nM Compound: GSK923295	Anticancer activity against human BT-474 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BT-474 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
BV-173	GI₅₀	56 nM Compound: GSK923295	Anticancer activity against human BV-173 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human BV-173 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
C-33-A	GI₅₀	47 nM Compound: GSK923295	Anticancer activity against human C-33-A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human C-33-A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
C3A	GI₅₀	54 nM Compound: GSK923295	Anticancer activity against human C3A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human C3A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
C-4-II	GI₅₀	46 nM Compound: GSK923295	Anticancer activity against human C-4-II cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human C-4-II cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CAKI-2	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human CAKI-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CAKI-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CAL-27	GI₅₀	47 nM Compound: GSK923295	Anticancer activity against human CAL-27 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CAL-27 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CAL-54	GI₅₀	49 nM Compound: GSK923295	Anticancer activity against human CAL-54 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CAL-54 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CAL-62	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human CAL-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CAL-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Capan-2	GI₅₀	119 nM Compound: GSK923295	Anticancer activity against human Capan-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Capan-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CCF-STTG1	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human CCF-STTG1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CCF-STTG1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CESS	GI₅₀	19 nM Compound: GSK923295	Anticancer activity against human CESS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CESS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CGTH-W-1	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human CGTH-W-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CGTH-W-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CHL-1	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human CHL-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CHL-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CHP-212	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human CHP-212 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CHP-212 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
COLO 201	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human COLO201 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human COLO201 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
COLO 205	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human COLO 205 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human COLO 205 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
COLO 320DM	GI₅₀	306 nM Compound: GSK923295	Anticancer activity against human COLO 320DM cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human COLO 320DM cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
COLO-320-HSR	GI₅₀	153 nM Compound: GSK923295	Anticancer activity against human COLO 320HSR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human COLO 320HSR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CRO-AP2	GI₅₀	51 nM Compound: GSK923295	Anticancer activity against human CRO-AP2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human CRO-AP2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
CWR22R	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human 22Rv1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human 22Rv1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
D283 Med	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human D283 Med cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human D283 Med cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DB	GI₅₀	21 nM Compound: GSK923295	Anticancer activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DBTRG-05MG	GI₅₀	17 nM Compound: GSK923295	Anticancer activity against human DBTRG-05MG cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DBTRG-05MG cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Detroit 562	GI₅₀	35 nM Compound: GSK923295	Anticancer activity against human Detroit 562 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Detroit 562 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DLD-1	GI₅₀	60 nM Compound: GSK923295	Anticancer activity against human DLD-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DLD-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DoTc2-4510	GI₅₀	33 nM Compound: GSK923295	Anticancer activity against human DoTc2-4510 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DoTc2-4510 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DU-145	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
DU-4475	GI₅₀	147 nM Compound: GSK923295	Anticancer activity against human DU-4475 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human DU-4475 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
EFM-19	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human EFM-19 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human EFM-19 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
EKVX	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human EKVX cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human EKVX cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
ES-2	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human ES2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human ES2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
FaDu	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human FaDu cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human FaDu cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
G-401	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human G-401 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human G-401 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
G-402	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human G-402 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human G-402 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
GCT	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human GCT cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human GCT cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
H4	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human H4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human H4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCC 2998	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human HCC 2998 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCC 2998 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCC1143	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human HCC1143 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCC1143 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCC1954	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human HCC1954 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCC1954 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCC70	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human HCC70 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCC70 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCT-116	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCT-15	GI₅₀	151 nM Compound: GSK923295	Anticancer activity against human HCT-15 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCT-15 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HCT-8	GI₅₀	35 nM Compound: GSK923295	Anticancer activity against human HCT-8 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HCT-8 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HEC-1-A	GI₅₀	50 nM Compound: GSK923295	Anticancer activity against human HEC-1-A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HEC-1-A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HeLa	GI₅₀	20 nM Compound: GSK923295	Anticancer activity against human HeLa cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HeLa cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Hep 3B2	GI₅₀	164 nM Compound: GSK923295	Anticancer activity against human Hep3B cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Hep3B cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HepG2	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HN5	GI₅₀	118 nM Compound: GSK923295	Anticancer activity against human HN5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HN5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HOP-62	GI₅₀	20 nM Compound: GSK923295	Anticancer activity against human HOP-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HOP-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HOS	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human HOS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HOS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HPAF-II	GI₅₀	5026 nM Compound: GSK923295	Anticancer activity against human HPAF-II cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HPAF-II cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HT-1080	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human HT-1080 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HT-1080 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HT-1376	GI₅₀	33 nM Compound: GSK923295	Anticancer activity against human HT-1376 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HT-1376 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HT-29	GI₅₀	14 nM Compound: GSK923295	Anticancer activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HT-3	GI₅₀	10000 nM Compound: GSK923295	Anticancer activity against human HT-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HT-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HuP-T4	GI₅₀	158 nM Compound: GSK923295	Anticancer activity against human HuP-T4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HuP-T4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
HuT78	GI₅₀	40 nM Compound: GSK923295	Anticancer activity against human HuT78 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human HuT78 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
IGROV-1	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human IGROV-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human IGROV-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
J82	GI₅₀	114 nM Compound: GSK923295	Anticancer activity against human J82 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human J82 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
JEG-3	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human JEG-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human JEG-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
K562	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
KM12	GI₅₀	56 nM Compound: GSK923295	Anticancer activity against human KM12 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human KM12 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
LNCaP	GI₅₀	76 nM Compound: GSK923295	Anticancer activity against human LNCaP cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human LNCaP cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
LOX IMVI	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human LOX IMVI cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human LOX IMVI cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
LS-1034	GI₅₀	97 nM Compound: GSK923295	Anticancer activity against human LS1034 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human LS1034 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
M14	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human M14 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human M14 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Malme-3M	GI₅₀	51 nM Compound: GSK923295	Anticancer activity against human Malme-3M cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Malme-3M cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MC-CAR	GI₅₀	86 nM Compound: GSK923295	Anticancer activity against human MC-CAR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MC-CAR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MCF-10A	GI₅₀	16 nM Compound: GSK923295	Anticancer activity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MCF7	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MC-IXC	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human MC-IXC cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MC-IXC cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MDA-MB-175-VII	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human MDA-MB-175-VII cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MDA-MB-175-VII cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MDA-MB-231	GI₅₀	5015 nM Compound: GSK923295	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MDA-MB-435	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human MDA-MB-435 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MDA-MB-435 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MDA-MB-453	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MDA-MB-468	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MES-SA	GI₅₀	65 nM Compound: GSK923295	Anticancer activity against human MES-SA cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MES-SA cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MIA PaCa-2	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human MIA PaCa-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MIA PaCa-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MOLT-16	GI₅₀	47 nM Compound: GSK923295	Anticancer activity against human MOLT-16 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MOLT-16 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MV4-11	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
MX1	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human MX1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human MX1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI/ADR-RES	GI₅₀	3962 nM Compound: GSK923295	Anticancer activity against human NCI/ADR-RES cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI/ADR-RES cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H1299	GI₅₀	52 nM Compound: GSK923295	Anticancer activity against human NCI-H1299 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H1299 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H146	GI₅₀	5226 nM Compound: GSK923295	Anticancer activity against human NCI-H146 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H146 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H157	GI₅₀	37 nM Compound: GSK923295	Anticancer activity against human NCI-H157 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H157 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H187	GI₅₀	68 nM Compound: GSK923295	Anticancer activity against human NCI-H187 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H187 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H2052	GI₅₀	44 nM Compound: GSK923295	Anticancer activity against human NCI-H2052 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H2052 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H209	GI₅₀	20 nM Compound: GSK923295	Anticancer activity against human NCI-H209 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H209 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H2122	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human NCI-H2122 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H2122 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H2170	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human NCI-H2170 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H2170 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H2171	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human NCI-H2171 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H2171 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H23	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human NCI-H23 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H23 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H292	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human NCI-H292 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H292 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H295R	GI₅₀	298 nM Compound: GSK923295	Anticancer activity against human NCI-H295R cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H295R cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H358	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human NCI-H358 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H358 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H460	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H508	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human NCI-H508 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H508 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H520	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human NCI-H520 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H520 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H526	GI₅₀	88 nM Compound: GSK923295	Anticancer activity against human NCI-H526 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H526 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H596	GI₅₀	5017 nM Compound: GSK923295	Anticancer activity against human NCI-H596 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H596 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H630	GI₅₀	47 nM Compound: GSK923295	Anticancer activity against human NCI-H630 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H630 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H661	GI₅₀	22 nM Compound: GSK923295	Anticancer activity against human NCI-H661 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H661 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H716	GI₅₀	174 nM Compound: GSK923295	Anticancer activity against human NCI-H716 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H716 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H747	GI₅₀	163 nM Compound: GSK923295	Anticancer activity against human NCI-H747 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H747 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-H82	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human NCI-H82 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-H82 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
NCI-N87	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human NCI-N87 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human NCI-N87 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
OV-90	GI₅₀	61 nM Compound: GSK923295	Anticancer activity against human OV-90 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human OV-90 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
OVCAR-3	GI₅₀	42 nM Compound: GSK923295	Anticancer activity against human OVCAR-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human OVCAR-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
OVCAR-4	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
OVCAR-5	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human OVCAR-5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human OVCAR-5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
OVCAR-8	GI₅₀	50 nM Compound: GSK923295	Anticancer activity against human OVCAR-8 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human OVCAR-8 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
PC-3	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Raji	GI₅₀	41 nM Compound: GSK923295	Anticancer activity against human Raji cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Raji cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RD	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human RD cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RD cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RKO	GI₅₀	53 nM Compound: GSK923295	Anticancer activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RL	GI₅₀	37 nM Compound: GSK923295	Anticancer activity against human RL cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RL cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RL95-2	GI₅₀	49 nM Compound: GSK923295	Anticancer activity against human RL95-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RL95-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RPMI-2650	GI₅₀	36 nM Compound: GSK923295	Anticancer activity against human RPMI-2650 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RPMI-2650 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RPMI-6666	GI₅₀	88 nM Compound: GSK923295	Anticancer activity against human RPMI-6666 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RPMI-6666 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RPMI-8226	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
RXF 393	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human RXF 393 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human RXF 393 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SAOS-2	GI₅₀	41 nM Compound: GSK923295	Anticancer activity against human SAOS-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SAOS-2 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SCaBER	GI₅₀	54 nM Compound: GSK923295	Anticancer activity against human SCaBER cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SCaBER cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SCC-15	GI₅₀	63 nM Compound: GSK923295	Anticancer activity against human SCC-15 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SCC-15 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SCC-25	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human SCC-25 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SCC-25 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SCC-4	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human SCC-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SCC-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SCC-9	GI₅₀	24 nM Compound: GSK923295	Anticancer activity against human SCC-9 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SCC-9 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SF-268	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human SF-268 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SF-268 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SF-295	GI₅₀	35 nM Compound: GSK923295	Anticancer activity against human SF-295 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SF-295 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SF-539	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human SF-539 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SF-539 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SH-4	GI₅₀	44 nM Compound: GSK923295	Anticancer activity against human SH-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SH-4 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SHP77	GI₅₀	86 nM Compound: GSK923295	Anticancer activity against human SHP77 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SHP77 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SiHa	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human SiHa cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SiHa cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SJRH30	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human SJRH30 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SJRH30 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-LMS-1	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human SK-LMS-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-LMS-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-MEL-28	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human SK-MEL-28 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-MEL-28 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-MEL3	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human SK-MEL3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-MEL3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-N-AS	GI₅₀	38 nM Compound: GSK923295	Anticancer activity against human SK-N-AS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-N-AS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-N-DZ	GI₅₀	69 nM Compound: GSK923295	Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-NEP-1	GI₅₀	55 nM Compound: GSK923295	Anticancer activity against human SK-NEP-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-NEP-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-N-FI	GI₅₀	120 nM Compound: GSK923295	Anticancer activity against human SK-N-FI cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-N-FI cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-OV-3	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SK-UT-1	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human SK-UT-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SK-UT-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SN12C	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human SN12C cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SN12C cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNB-19	GI₅₀	28 nM Compound: GSK923295	Anticancer activity against human SNB-19 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNB-19 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNB-75	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human SNB-75 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNB-75 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU1	GI₅₀	10000 nM Compound: GSK923295	Anticancer activity against human SNU1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-16	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human SNU-16 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-16 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-387	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human SNU-387 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-387 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-398	GI₅₀	27 nM Compound: GSK923295	Anticancer activity against human SNU-398 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-398 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-423	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human SNU-423 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-423 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-449	GI₅₀	236 nM Compound: GSK923295	Anticancer activity against human SNU-449 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-449 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-475	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human SNU-475 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-475 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SNU-5	GI₅₀	88 nM Compound: GSK923295	Anticancer activity against human SNU-5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SNU-5 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SR	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human SR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SR cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
ST486	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human ST486 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human ST486 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW 954	GI₅₀	22 nM Compound: GSK923295	Anticancer activity against human SW 954 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW 954 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW 962	GI₅₀	21 nM Compound: GSK923295	Anticancer activity against human SW 962 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW 962 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW1088	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human SW1088 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW1088 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW1417	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human SW1417 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW1417 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW1463	GI₅₀	31 nM Compound: GSK923295	Anticancer activity against human SW1463 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW1463 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW1783	GI₅₀	34 nM Compound: GSK923295	Anticancer activity against human SW1783 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW1783 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW1990	GI₅₀	127 nM Compound: GSK923295	Anticancer activity against human SW1990 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW1990 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW48	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human SW48 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW48 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW480	GI₅₀	33 nM Compound: GSK923295	Anticancer activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW-620	GI₅₀	47 nM Compound: GSK923295	Anticancer activity against human SW620 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW620 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW684	GI₅₀	5016 nM Compound: GSK923295	Anticancer activity against human SW684 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW684 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW756	GI₅₀	35 nM Compound: GSK923295	Anticancer activity against human SW756 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW756 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW780	GI₅₀	30 nM Compound: GSK923295	Anticancer activity against human SW780 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW780 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW837	GI₅₀	33 nM Compound: GSK923295	Anticancer activity against human SW837 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW837 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW872	GI₅₀	37 nM Compound: GSK923295	Anticancer activity against human SW872 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW872 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
SW948	GI₅₀	98 nM Compound: GSK923295	Anticancer activity against human SW948 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human SW948 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
T-24	GI₅₀	45 nM Compound: GSK923295	Anticancer activity against human T24 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human T24 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
T47D	GI₅₀	29 nM Compound: GSK923295	Anticancer activity against human T47D cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human T47D cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
T84	GI₅₀	75 nM Compound: GSK923295	Anticancer activity against human T84 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human T84 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
THP-1	GI₅₀	12 nM Compound: GSK923295	Anticancer activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
TK-10	GI₅₀	49 nM Compound: GSK923295	Anticancer activity against human TK-10 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human TK-10 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
U-251	GI₅₀	26 nM Compound: GSK923295	Anticancer activity against human U-251 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human U-251 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
U2OS	GI₅₀	45 nM Compound: GSK923295	Anticancer activity against human U2OS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human U2OS cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
UACC-257	GI₅₀	32 nM Compound: GSK923295	Anticancer activity against human UACC-257 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human UACC-257 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
UACC-62	GI₅₀	25 nM Compound: GSK923295	Anticancer activity against human UACC-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human UACC-62 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
UMUC3	GI₅₀	23 nM Compound: GSK923295	Anticancer activity against human UM-UC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human UM-UC-3 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
WiDr	GI₅₀	18 nM Compound: GSK923295	Anticancer activity against human WiDr cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human WiDr cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
Y79	GI₅₀	70 nM Compound: GSK923295	Anticancer activity against human Y79 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human Y79 cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]
YAPC	GI₅₀	59 nM Compound: GSK923295	Anticancer activity against human YAPC cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis Anticancer activity against human YAPC cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis	[PMID: 20167803]

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 K_i 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 K_i 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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In 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)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1088965-37-0
Appearance Solid
Molecular Weight 592.13
Formel C₃₂H₃₈ClN₅O₄
Color White to yellow
SMILES

O=C(N[C@@H](CC1=CC=C(C2=CN3C(C([C@@H](O)C)=CC=C3)=N2)C=C1)CNC(CN(C)C)=O)C4=CC(Cl)=C(C=C4)OC(C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (41)

All WB

Sort by:

Journal Impact Factor

Science

Mitosis. Microtubule detyrosination guides chromosomes during mitosis. [Abstract]

2015 May 15;348(6236):799-803. PMID: 25908662
Science

Spatial organization of cytokinesis signaling reconstituted in a cell-free system. [Abstract]

2014 Oct 10;346(6206):244-7. PMID: 25301629
Nat Cell Biol

Adaptive changes in the kinetochore architecture facilitate proper spindle assembly. [Abstract]

2015 Sep;17(9):1134-44. PMID: 26258631
Nat Cell Biol

Kinetochore motors drive congression of peripheral polar chromosomes by overcoming random arm-ejection forces. [Abstract]

2014 Dec;16(12):1249-56. PMID: 25383660
Nat Cell Biol

CLASPs prevent irreversible multipolarity by ensuring spindle-pole resistance to traction forces during chromosome alignment. [Abstract]

2012 Feb 5;14(3):295-303. PMID: 22307330
Nat Commun

Polar chromosomes are rescued from missegregation by spindle elongation-driven microtubule pivoting. [Abstract]

2026 Mar 17;17(1):2049. PMID: 41844586
Nat Commun

Chk2 sustains PLK1 activity in mitosis to ensure proper chromosome segregation. [Abstract]

2024 Dec 30;15(1):10782. PMID: 39737931
Nat Commun

α-tubulin detyrosination fine-tunes kinetochore-microtubule attachments. [Abstract]

2024 Nov 9;15(1):9720. PMID: 39521805
Cancer Lett

Pgp efflux pump decreases the cytostatic effect of CENP-E inhibitor GSK923295. [Abstract]

2015 May 28;361(1):97-103. PMID: 25725449

GSK-923295 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2015 May 28;361(1):97-103. [Abstract]

Apoptotic effects of GSK923295 on MESSA and MESSA Dx5 cells. MESSA and MESSA Dx5 cells are treated with Verapamil (20 μM), GSK923295 (4 μM), and combination GSK923295 (4 μM) plus Verapamil (20 μM) for 24 h. Actin is used as loading control.
Cell Death Discov

Kinesin-7 CENP-E regulates chromosome alignment and genome stability of spermatogenic cells. [Abstract]

2020 Apr 20;6:25. PMID: 32351712
Dev Cell

Microtubule-sliding modules based on kinesins EG5 and PRC1-dependent KIF4A drive human spindle elongation. [Abstract]

2021 May 3;56(9):1253-1267.e10. PMID: 33910056
Cell Chem Biol

Distinct Mechanisms of Resistance to a CENP-E Inhibitor Emerge in Near-Haploid and Diploid Cancer Cells. [Abstract]

2020 Jul 16;27(7):850-857.e6. PMID: 32442423
Curr Biol

Non-centrosomal microtubules at kinetochores promote rapid chromosome biorientation during mitosis in human cells. [Abstract]

2022 Mar 14;32(5):1049-1063.e4. PMID: 35108523
Curr Biol

Lateral to end-on conversion of chromosome-microtubule attachment requires kinesins CENP-E and MCAK. [Abstract]

2013 Aug 19;23(16):1514-26. PMID: 23891108
Cell Prolif

Kinesin-7 CENP-E mediates centrosome organization and spindle assembly to regulate chromosome alignment and genome stability. [Abstract]

2024 Sep 12:e13745. PMID: 39266203
Pharmaceutics

Maximizing Anticancer Response with MPS1 and CENPE Inhibition Alongside Apoptosis Induction. [Abstract]

2023 Dec 29;16(1):56. PMID: 38258067
J Cell Biol

Deep learning techniques and mathematical modeling allow 3D analysis of mitotic spindle dynamics. [Abstract]

2023 May 1;222(5):e202111094. PMID: 36880744
J Cell Biol

Small changes in phospho-occupancy at the kinetochore-microtubule interface drive mitotic fidelity. [Abstract]

2022 Sep 5;221(9). PMID: 35878017
J Cell Biol

Microtubules assemble near most kinetochores during early prometaphase in human cells. [Abstract]

2018 Aug 6;217(8):2647-2659. PMID: 29907657
J Cell Biol

Spindle assembly checkpoint satisfaction occurs via end-on but not lateral attachments under tension. [Abstract]

2017 Jun 5;216(6):1533-1542. PMID: 28536121
J Cell Biol

Dynein light intermediate chains maintain spindle bipolarity by functioning in centriole cohesion. [Abstract]

2014 Nov 24;207(4):499-516. PMID: 25422374
Mol Cancer Res

Overlaid Transcriptional and Proteome Analyses Identify Mitotic Kinesins as Important Targets of Arylsulfonamide-Mediated RBM39 Degradation. [Abstract]

2023 Aug 1;21(8):768-778. PMID: 37255411
Biochim Biophys Acta Mol Cell Res

Kinesin-7 CENP-E is essential for chromosome alignment and spindle assembly of mouse spermatocytes. [Abstract]

2022 Sep;1869(9):119306. PMID: 35680098
Eur J Cell Biol

Kinesin-7 CENP-E regulates cell division, gastrulation and organogenesis in development. [Abstract]

2020 Aug;99(6):151107. PMID: 32800279
Cell Cycle

Dynein prevents erroneous kinetochore-microtubule attachments in mitosis. [Abstract]

2015 Nov 2;14(21):3356-61. PMID: 26397382
J Cell Sci

Chromosome congression is promoted by CENP-Q- and CENP-E-dependent pathways. [Abstract]

2015 Jan 1;128(1):171-84. PMID: 25395579
Breast Cancer Res Treat

Molecular determinants of drug response in TNBC cell lines. [Abstract]

2020 Jan;179(2):337-347. PMID: 31655920
Cell Tissue Res

Kinesin-7 CENP-E regulates the formation and structural maintenance of the acrosome. [Abstract]

2021 Mar;383(3):1167-1182. PMID: 33237480
Biochem Biophys Res Commun

Identification of benzo[d]pyrrolo[2,1-b]thiazole derivatives as CENP-E inhibitors. [Abstract]

2019 Nov 12;519(3):505-511. PMID: 31530389
bioRxiv

2026 Apr 5.
bioRxiv

2025 Sep 13.
bioRxiv

2024 August 30.
bioRxiv

2024 October 01.
bioRxiv

Proximity-based activation of AURORA A by MPS1 potentiates error correction. [Abstract]

2024 Jun 13:2024.06.11.598300. PMID: 38948877
bioRxiv

2023 Nov 10.
bioRxiv

An Aurora kinase A-BOD1L1-PP2A B56 Axis promotes chromosome segregation fidelity. [Abstract]

2024 Mar 6:2023.08.06.552174. PMID: 37609141
bioRxiv

2021 Feb 1.
University of California

2019 Jun.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898
Oncotarget

Heterogeneity in sarcoma cell lines reveals enhanced motility of tetraploid versus diploid cells. [Abstract]

2017 Mar 7;8(10):16669-16689. PMID: 28035071
Chem Biol

Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. [Abstract]

2011 Jun 24;18(6):679-80. PMID: 21700202

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 60 mg/mL (101.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6888 mL

8.4441 mL

16.8882 mL

5 mM

0.3378 mL

1.6888 mL

3.3776 mL

10 mM

0.1689 mL

0.8444 mL

1.6888 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

Cell-growth inhibition assays are performed by MDS in 384-well plates, and DNA content of fixed cells stained with DAPI using an Incell 1000 (GE) is analyzed. DNA content is determined 24 h after seeding (T₀) and after exposure to varying concentrations of GSK-923295 (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, and 100 μM) for an additional 72 h (T₇₂). All T₇₂ measurements are normalized to T₀. Curves are analyzed using the XLfit curve-fitting tool to determine the concentration of GSK923295 yielding 50% growth inhibition relative to T₀ and Y_max values (GI₅₀)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
CB17 scid mice are used to propagate subcutaneously implanted neuroblastoma tumors. Tumor diameters are measured using calipers. Tumor volumes are calculated. Once tumor volume exceeds 200 mm³, mice are randomized (n=10 per arm) to receive either GSK923295 125 mg/kg IP or vehicle (96% acidified water, 2% DMAC, 2% CREM) for a total of 6 doses using a 3 days on, 4 days off, 3 days on regimen.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6888 mL	8.4441 mL	16.8882 mL	42.2205 mL
	5 mM	0.3378 mL	1.6888 mL	3.3776 mL	8.4441 mL
	10 mM	0.1689 mL	0.8444 mL	1.6888 mL	4.2220 mL
	15 mM	0.1126 mL	0.5629 mL	1.1259 mL	2.8147 mL
	20 mM	0.0844 mL	0.4222 mL	0.8444 mL	2.1110 mL
	25 mM	0.0676 mL	0.3378 mL	0.6755 mL	1.6888 mL
	30 mM	0.0563 mL	0.2815 mL	0.5629 mL	1.4073 mL
	40 mM	0.0422 mL	0.2111 mL	0.4222 mL	1.0555 mL
	50 mM	0.0338 mL	0.1689 mL	0.3378 mL	0.8444 mL
	60 mM	0.0281 mL	0.1407 mL	0.2815 mL	0.7037 mL
	80 mM	0.0211 mL	0.1056 mL	0.2111 mL	0.5278 mL
	100 mM	0.0169 mL	0.0844 mL	0.1689 mL	0.4222 mL

Keywords

GSK-923295

41 Cited Publications

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GSK-923295

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK-923295

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (41)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK-923295

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK-923295

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (41)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK-923295 Related Classifications

HY-10299 Related Classifications