proTAME 5μM R04 exp187

proTAME 5μM R04 exp187

Mechanism of Action

Inhibits APC/C interaction with Cdc20/Cdh1 substrate recognition cofactors

Class / Subclass 1: Proteostasis / E3 ubiquitin ligase inhibitor
Class / Subclass 2: Cell Cycle / Mitotic Inhibitor

Technical Notes

Compound References

PubChem Name: Methyl (2S)-5-[bis[(2-phenylacetyl)oxymethoxycarbonylamino]methylideneamino]-2-[(4-methylphenyl)sulfonylamino]pentanoate
Synonyms: N/A
CAS #: 1362911-19-0
PubChem CID: 56924780
IUPAC: methyl (2S)-5-[bis[(2-phenylacetyl)oxymethoxycarbonylamino]methylideneamino]-2-[(4-methylphenyl)sulfonylamino]pentanoate
INCHI Name: InChI=1S/C34H38N4O12S/c1-24-15-17-27(18-16-24)51(44,45)38-28(31(41)46-2)14-9-19-35-32(36-33(42)49-22-47-29(39)20-25-10-5-3-6-11-25)37-34(43)50-23-48-30(40)21-26-12-7-4-8-13-26/h3-8,10-13,15-18,28,38H,9,14,19-23H2,1-2H3,(H2,35,36,37,42,43)/t28-/m0/s1
INCHI Key: MHYOVHULCQSDRZ-NDEPHWFRSA-N
Molecular Weight: 726.8
Canonical SMILES: CC1=CC=C(C=C1)S(=O)(=O)NC(CCCN=C(NC(=O)OCOC(=O)CC2=CC=CC=C2)NC(=O)OCOC(=O)CC3=CC=CC=C3)C(=O)OC
Isomeric SMILES: CC1=CC=C(C=C1)S(=O)(=O)N[C@@H](CCCN=C(NC(=O)OCOC(=O)CC2=CC=CC=C2)NC(=O)OCOC(=O)CC3=CC=CC=C3)C(=O)OC
Molecular Formula: C34H38N4O12S

Compound Supplier

Supplier Name: Boston Biochem
Catalog #: I-440
Lot #: N/A

Compound Characterization

LCMS: Tr 1.24 min, m/z 203-

Dose Response Curve

Platform ID: proTAME
Min: -10.5981; Max: 74.8880

IC	Concentration (µM)
IC10	N/A
IC20	16.3280
IC30	17.0911
IC40	17.7431
IC50	18.3634
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 04
Dose: 5µM
Days of incubation: 8
Doublings: 6.7
Numbers of reads: 19315630

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
12/3	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
TRIP13	-4.23	<0.01
MAD2L1BP	-3.96	<0.01
ANAPC7	-3.96	<0.01
SLC18B1	-3.78	<0.01
ARL1	-3.52	<0.01
UBE2S	-3.39	<0.01
KDSR	-3.27	<0.01
ANAPC16	-2.90	<0.01
GCLM	-2.67	0.01
ZFAT	-2.66	0.03
NPRL2	-2.60	0.02
PGGT1B	-2.60	0.02
ANAPC13	-2.54	0.05
TCF4	-2.39	0.05
ALG3	-2.38	0.05
ALDH18A1	-2.37	0.05
MAPK14	-2.36	0.05
ALG6	-2.35	0.05
ANAPC15	-2.34	0.15
RUNX3	-2.33	0.05
KCTD5	-2.33	0.05
MCM9	-2.31	0.05
C17orf70	-2.29	0.06
MCTS1	-2.23	0.08
SEPSECS	-2.22	0.14
UBE2C	-2.21	0.09
GTF3C6	-2.19	0.09
SEC62	-2.17	0.16
C1orf27	-2.15	0.11
KIAA1432	-2.12	0.12
GPR108	1.99	0.50
PCDHB5	2.00	0.47
INTS5	2.01	0.60
RPL34	2.01	0.62
ZP3	2.05	0.47
DDX41	2.05	0.47
CHCHD5	2.08	0.46
SRSF3	2.09	0.47
NID2	2.13	0.47
RPL37A	2.14	0.62
DDX47	2.21	0.67
NOP16	2.21	0.57
PCDHB1	2.22	0.30
CKAP5	2.24	0.57
MYB	2.24	0.50
HIVEP3	2.26	0.47
WDR75	2.30	0.47
MYH13	2.36	0.46
TMEM74	2.37	0.15
SLC24A2	2.37	0.46
PARP3	2.48	0.09
RNF112	2.64	0.09
SART1	2.72	0.50
TBC1D3I	2.83	0.47
TBC1D3E	2.84	0.47
TBC1D3K	2.84	0.47
TBC1D3L	2.85	0.47
ZNF653	3.05	0.01
NCEH1	4.29	<0.01
ABHD6	4.90	<0.01

Screen	Correlation	Plot
Apcin 25μM plus proTAME 2μM R04 exp177	0.148	View
Apcin 50 to 100μM on day4 R04 exp176	0.095	View
Prochlorperazine 5.2μM R02 exp77	0.062	View
BH1 1μM R04 exp169	0.056	View
L-BMAA 500 to 750μM on day4 R04 exp185	0.054	View
Ixabepilone 0.004 to 0.005μM on day4 R04 exp184	0.054	View
UM0130462 0.025 to 0.035μM day4 R05 exp247	0.052	View

GO Term	Fold Change	Genes
anaphase-promoting complex	184.16	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,UBE2C
anaphase-promoting complex-dependent catabolic process	184.16	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,UBE2C
positive regulation of mitotic metaphase/anaphase transition	141.66	MAD2L1BP,ANAPC7,UBE2C
positive regulation of metaphase/anaphase transition of cell cycle	131.54	MAD2L1BP,ANAPC7,UBE2C
positive regulation of mitotic sister chromatid separation	108.33	MAD2L1BP,ANAPC7,UBE2C
protein K11-linked ubiquitination	87.69	ANAPC7,UBE2S,ANAPC13,UBE2C
nuclear ubiquitin ligase complex	85.65	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,UBE2C
regulation of mitotic sister chromatid separation	52.92	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of meiotic cell cycle	48.72	TRIP13,ANAPC7,ANAPC16,ANAPC13,ANAPC15
regulation of chromosome separation	42.04	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of mitotic metaphase/anaphase transition	34.49	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of metaphase/anaphase transition of cell cycle	33.36	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of sister chromatid segregation	29.80	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of mitotic nuclear division	26.23	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
regulation of chromosome segregation	24.36	TRIP13,MAD2L1BP,ANAPC7,ANAPC15,UBE2C
cullin-RING ubiquitin ligase complex	23.87	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,KCTD5,UBE2C
ubiquitin ligase complex	13.82	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,KCTD5,UBE2C
proteasome-mediated ubiquitin-dependent protein catabolic process	12.45	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,KCTD5,UBE2C
proteasomal protein catabolic process	11.31	ANAPC7,UBE2S,ANAPC16,ANAPC13,ANAPC15,KCTD5,UBE2C

Table of Contents

proTAME 5μM R04 exp187

Mechanism of Action

Technical Notes

Compound References

Compound Supplier

Compound Characterization

Dose Response Curve

Screen Summary

Screen Results