Apcin 50 to 100μM on day4 R04 exp176

Apcin 50 to 100μM on day4 R04 exp176

Mechanism of Action

Inhibits substrate interactions with APC/C-Cdc20

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

Technical Notes

Protein References

PubChem Name: Apcin
Synonyms: N/A
CAS #: 300815-04-7
PubChem CID: 2830389
IUPAC: 2-(2-methyl-5-nitroimidazol-1-yl)ethyl N-[2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl]carbamate
INCHI Name: InChI=1S/C13H14Cl3N7O4/c1-8-19-7-9(23(25)26)22(8)5-6-27-12(24)21-10(13(14,15)16)20-11-17-3-2-4-18-11/h2-4,7,10H,5-6H2,1H3,(H,21,24)(H,17,18,20)
INCHI Key: ZEXHXVOGJFGTRX-UHFFFAOYSA-N
Molecular Weight: 438.6
Canonical SMILES: CC1=NC=C(N1CCOC(=O)NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)[N+](=O)[O-]
Isomeric SMILES: N/A
Molecular Formula: C13H14Cl3N7O4

Protein Supplier

Supplier Name: Boston Biochem
Catalog #: I-444
Lot #: N/A

Protein Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C13H14Cl3N7O4 438.02456; found 438.02545

Dose Response Curve

Platform ID: Apcin
Min: -13.2600; Max: 16.4769

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

Screen Summary

Round: 04
Dose: 50-100µM
Days of incubation: 8
Doublings: 6.8
Numbers of reads: 17845743

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
14/1	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
UBE2S	-4.33	<0.01
OTUB1	-4.24	<0.01
ANAPC7	-4.11	<0.01
KIF20A	-4.10	<0.01
UBE2C	-3.52	<0.01
CCNB1	-3.39	<0.01
ANAPC13	-3.27	<0.01
SCAP	-2.76	<0.01
KCTD5	-2.63	0.02
BEX5	-2.62	0.02
SEPSECS	-2.60	0.04
PIK3R4	-2.50	0.03
BRD1	-2.44	0.04
DNAJC8	-2.40	0.05
PMM2	-2.36	0.06
SLC5A6	-2.34	0.06
IPO13	-2.29	0.12
KIAA1432	-2.27	0.08
ANAPC15	-2.27	0.21
DAXX	-2.22	0.16
ESPL1	-2.22	0.58
QRICH1	-2.20	0.24
CKS2	-2.20	0.11
NPRL2	-2.20	0.11
PGGT1B	-2.17	0.12
ADNP	-2.17	0.12
MEDAG	-2.16	0.12
DPH1	-2.13	0.13
MNS1	-2.08	0.23
EIF4A1	-2.05	0.19
ERCC6L2	1.95	0.49
POLR3G	1.96	0.51
PLXNB1	1.97	0.49
TTYH1	1.99	0.51
GPR101	2.01	0.49
RANBP2	2.02	0.49
RSL1D1	2.03	0.49
HOXA7	2.04	0.40
ROBO4	2.04	0.49
C9orf170	2.09	0.49
STAT4	2.10	0.32
ANKRD23	2.16	0.40
HTRA2	2.18	0.26
POLD3	2.22	0.71
SYT14	2.23	0.22
RPL30	2.25	0.73
CSAD	2.26	0.21
UTP18	2.26	0.29
HTR1B	2.29	0.27
AQR	2.30	0.59
NPIPA8	2.34	0.15
KPNB1	2.35	0.57
NPIPA7	2.35	0.15
TUBGCP2	2.37	0.15
PHB2	2.40	0.56
PALM	2.45	0.15
CACNA1A	2.48	0.15
POLA2	2.68	0.53
KRT78	2.74	0.13
PAQR6	3.19	0.02

Screen	Correlation	Plot
proTAME 5μM R04 exp187	0.095	View
Apcin 25μM plus proTAME 2μM R04 exp177	0.094	View

GO Term	Fold Change	Genes
anaphase-promoting complex	147.98	UBE2S,ANAPC7,UBE2C,ANAPC13,ANAPC15
anaphase-promoting complex-dependent catabolic process	147.98	UBE2S,ANAPC7,UBE2C,ANAPC13,ANAPC15
positive regulation of metaphase/anaphase transition of cell cycle	126.84	ANAPC7,UBE2C,ESPL1
positive regulation of mitotic sister chromatid separation	104.46	ANAPC7,UBE2C,ESPL1
protein K11-linked ubiquitination	84.56	UBE2S,ANAPC7,UBE2C,ANAPC13
nuclear ubiquitin ligase complex	68.83	UBE2S,ANAPC7,UBE2C,ANAPC13,ANAPC15
regulation of mitotic sister chromatid separation	51.03	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of chromosome separation	40.54	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of mitotic metaphase/anaphase transition	33.25	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of metaphase/anaphase transition of cell cycle	32.17	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of sister chromatid segregation	28.73	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of mitotic nuclear division	25.30	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
regulation of chromosome segregation	23.49	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
cullin-RING ubiquitin ligase complex	23.02	UBE2S,ANAPC7,UBE2C,ANAPC13,KCTD5,ANAPC15,CKS2
regulation of nuclear division	20.55	ANAPC7,UBE2C,CCNB1,ANAPC15,ESPL1
ubiquitin ligase complex	13.32	UBE2S,ANAPC7,UBE2C,ANAPC13,KCTD5,ANAPC15,CKS2
cell division	10.53	UBE2S,ANAPC7,KIF20A,UBE2C,CCNB1,ANAPC13,ANAPC15,ESPL1,CKS2
transferase complex	7.86	UBE2S,ANAPC7,UBE2C,CCNB1,ANAPC13,KCTD5,PIK3R4,BRD1,ANAPC15,CKS2,PGGT1B
intracellular protein-containing complex	6.76	UBE2S,ANAPC7,UBE2C,ANAPC13,KCTD5,BRD1,RIC1,ANAPC15,CKS2,PGGT1B

Table of Contents

Apcin 50 to 100μM on day4 R04 exp176

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results