Taxol 0.004μM R03 exp103

Taxol 0.004μM R03 exp103

Mechanism of Action

Inhibits microtubule depolymerisation, blocks metaphase to anaphase transition

Class / Subclass 1: Cell Cycle / Microtubule Poison
Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor

Technical Notes

Protein References

PubChem Name: Paclitaxel
Synonyms: Taxol
CAS #: 33069-62-4
PubChem CID: 36314
IUPAC: [(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-15-[(2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl]oxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
INCHI Name: InChI=1S/C47H51NO14/c1-25-31(60-43(56)36(52)35(28-16-10-7-11-17-28)48-41(54)29-18-12-8-13-19-29)23-47(57)40(61-42(55)30-20-14-9-15-21-30)38-45(6,32(51)22-33-46(38,24-58-33)62-27(3)50)39(53)37(59-26(2)49)34(25)44(47,4)5/h7-21,31-33,35-38,40,51-52,57H,22-24H2,1-6H3,(H,48,54)/t31-,32-,33+,35-,36+,37+,38-,40-,45+,46-,47+/m0/s1
INCHI Key: RCINICONZNJXQF-MZXODVADSA-N
Molecular Weight: 853.9
Canonical SMILES: CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)C6=CC=CC=C6)O)O)OC(=O)C7=CC=CC=C7)(CO4)OC(=O)C)O)C)OC(=O)C
Isomeric SMILES: CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)C6=CC=CC=C6)O)O)OC(=O)C7=CC=CC=C7)(CO4)OC(=O)C)O)C)OC(=O)C
Molecular Formula: C47H51NO14

Protein Supplier

Supplier Name: LC Laboratories
Catalog #: P-9600
Lot #: N/A

Protein Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C47H51NO14 854.33823; found 854.33694

Dose Response Curve

Platform ID: Taxol
Min: -3.3721; Max: 85.0520

IC	Concentration (µM)
IC10	N/A
IC20	0.0020
IC30	0.0023
IC40	0.0025
IC50	0.0028
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 03
Dose: 4nM
Days of incubation: 8
Doublings: 5.1
Numbers of reads: 13302692

Screen Results

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
37/35	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
KIF18B	-5.38	<0.01
KIF2C	-4.17	<0.01
TACC3	-3.81	<0.01
SEPHS1	-3.55	<0.01
UBE4B	-3.55	<0.01
KIF2A	-3.27	<0.01
GAK	-3.21	<0.01
PPP2R5C	-3.15	<0.01
DLGAP5	-3.10	<0.01
KATNA1	-3.00	<0.01
KATNB1	-2.98	<0.01
RUVBL1	-2.94	0.11
KMT2D	-2.90	<0.01
NEDD1	-2.82	0.03
MSI2	-2.80	<0.01
KLF16	-2.78	0.02
MCTS1	-2.75	<0.01
CNOT2	-2.71	<0.01
KIF4A	-2.69	<0.01
PPME1	-2.68	0.03
GNA13	-2.64	<0.01
TRIP13	-2.63	0.02
ELAVL1	-2.60	0.01
KEAP1	-2.60	0.01
GTSE1	-2.59	0.01
CDCA2	-2.58	0.01
SMEK1	-2.57	0.01
ANP32A	-2.53	0.03
HMMR	-2.48	0.03
MAP4	-2.48	0.03
ZNF280D	2.50	0.01
HOXC10	2.50	0.11
PPP1CC	2.51	0.01
CHD7	2.51	0.03
PNPLA8	2.52	0.05
PRKRIR	2.52	0.01
CRKL	2.56	0.02
MBNL1	2.56	0.01
PFDN4	2.57	0.01
TP53BP1	2.60	0.01
UFC1	2.63	0.01
MED13L	2.74	0.01
ATF6	2.75	0.01
C4orf29	2.79	<0.01
SSSCA1	2.79	<0.01
TMEM126B	2.82	<0.01
PFDN5	2.96	<0.01
UFSP2	3.17	<0.01
MAPKAPK5	3.19	<0.01
SLC4A7	3.25	<0.01
SLAIN1	3.34	<0.01
VBP1	3.37	<0.01
COPS7B	3.48	<0.01
TP53	3.79	<0.01
TUBA1B	4.28	<0.01
SAMHD1	4.50	<0.01
CLASP1	4.73	<0.01
FBXO11	5.41	<0.01
AHCYL1	5.95	<0.01
KIFC1	6.29	<0.01

Screen	Correlation	Plot
Vincristine 0.0005μM R04 exp190	0.084	View
UMK57 1μM R01 exp59	0.078	View
UM131593 0.2μM R03 exp106	0.062	View
Vinblastine 0.002μM R01 exp60	0.056	View
Ixabepilone 0.004 to 0.005μM on day4 R04 exp184	0.181	View
Epothilone-B 0.0015μM R05 exp231	0.155	View
BML-284 0.09μM R08 exp460	0.109	View
Mdivi-1 15μM R05 exp217	0.104	View
Cabazitaxel 0.001μM R05 exp223	0.096	View
Docetaxel 0.002μM R01 exp45	0.083	View
Combretastatin A4 0.002 to 0.003μM day4 R04 exp179	0.076	View
Quercetin 20μM R08 exp517	0.075	View
Demecolcine 0.03μM R05 exp228	0.066	View
Sulforaphane 9μM R08 exp525	0.066	View
Sulforaphane 9μM R08 exp526 no dilution day6	0.062	View
Colchicine 0.009μM R05 exp215	0.06	View
Docetaxel 0.001 to 0.002μM on day4 R04 exp159	0.059	View
BI-2536 0.0042μM R03 exp95	0.057	View
LY2090314 0.003μM R08 exp500 no dilution day6	0.056	View
HMS-I1 1μM R01 exp46	0.053	View
S-trityl-L-cysteine 0.5μM R05 exp243	0.051	View

GO Term	Fold Change	Genes
protein depolymerization	75.22	KIF18B,KIF2C,KIF2A,GAK,KATNB1
mitotic sister chromatid segregation	25.04	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,KIF4A
sister chromatid segregation	24.33	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,KIF4A
mitotic nuclear division	20.92	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,KIF4A
spindle pole	20.18	TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1
nuclear chromosome segregation	18.19	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,KIF4A,TRIP13
microtubule binding	17.26	KIF18B,KIF2C,KIF2A,DLGAP5,KATNA1,KATNB1,KIF4A,GTSE1
tubulin binding	14.06	KIF18B,KIF2C,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1,KIF4A,GTSE1
chromosome segregation	13.94	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,KIF4A,TRIP13,CDCA2
spindle	13.78	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1,KIF4A,HMMR
cell division	11.30	KIF18B,KIF2C,TACC3,KIF2A,KATNA1,KATNB1,RUVBL1,NEDD1,KIF4A,CDCA2
mitotic cell cycle process	11.06	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNB1,KIF4A,PPME1,TRIP13,GTSE1
mitotic cell cycle	10.46	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNB1,NEDD1,KIF4A,PPME1,TRIP13,GTSE1
chromosome organization	10.37	KIF18B,KIF2C,KIF2A,DLGAP5,KATNB1,RUVBL1,KIF4A,TRIP13
microtubule cytoskeleton organization	9.53	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1,KIF4A
centrosome	8.35	KIF2C,TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1,KEAP1,HMMR
microtubule organizing center	7.79	KIF2C,TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,RUVBL1,NEDD1,KEAP1,PPP4R3A,HMMR
microtubule-based process	7.32	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNA1,KATNB1,NEDD1,KIF4A,GTSE1
cell cycle process	7.20	KIF18B,KIF2C,TACC3,KIF2A,DLGAP5,KATNB1,KIF4A,PPME1,TRIP13,GTSE1,CDCA2

Table of Contents

Taxol 0.004μM R03 exp103

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results