Bortezomib 0.05μM R00 exp7

Inhibits 26S proteasome, binds reversibly to chymotrypsin-like catalytic sites

PubChem Name: Bortezomib
Synonyms: PS-341; Brotezamide; DPBA; LDP 341; MG 341; Radiciol; NSC 681239
CAS #: 179324-69-7
PubChem CID: 387447
IUPAC: [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
INCHI Name: InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
INCHI Key: GXJABQQUPOEUTA-RDJZCZTQSA-N
Molecular Weight: 384.2
Canonical SMILES: B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Isomeric SMILES: B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Molecular Formula: C19H25BN4O4

HRMS (ESI-TOF) m/z: [M+H-H2O]+ Calcd for C19H24BN4O3 367.1936; found 367.1966

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
31/20	Scores	View	View	View	View	View

Screen	Correlation	Plot
DABN 20μM R00 exp17	0.119	View
Pimelic-diphenylamide-106 5μM R00 exp28	0.102	View
Etoposide 1μM R00 exp19	0.095	View
MLN-4924 2μM R00 exp22	0.092	View
Rotenone 20μM R00 exp34	0.086	View
Oligomycin-A 20μM R00 exp26	0.072	View
Brefeldin A 0.02μM R00 exp8	0.072	View
Etoposide 0.3μM R05 exp199	0.058	View
Nocodazole 0.2μM R00 exp24	0.055	View
GSK461364A 0.1μM R03 exp126	0.055	View
Q15 2.7μM R02 exp79	0.051	View
Dorsomorphin 5μM R07 exp357	0.051	View
5-Fluorouracil 20μM R00 exp2	0.088	View
Actinomycin-D 0.001μM R00 exp3	0.074	View
Actinomycin-D 0.01μM R00 exp4	0.072	View

GO Term	Fold Change	Genes
GARP complex	394.79	VPS51,VPS52
proton-transporting ATPase activity, rotational mechanism	77.24	ATP6V0A2,ATP6V1B2,ATP6V1A
ATPase-coupled ion transmembrane transporter activity	77.24	ATP6V0A2,ATP6V1B2,ATP6V1A
ATPase activity, coupled to transmembrane movement of ions, rotational mechanism	77.24	ATP6V0A2,ATP6V1B2,ATP6V1A
vacuolar proton-transporting V-type ATPase complex	74.02	ATP6V0A2,ATP6V1B2,ATP6V1A
proton-transporting V-type ATPase complex	65.80	ATP6V0A2,ATP6V1B2,ATP6V1A
vacuolar acidification	53.83	ATP6V0A2,ATP6V1B2,ATP6V1A
vesicle tethering complex	43.87	VPS51,COG3,VPS52,COG1
trans-Golgi network membrane	23.22	VPS51,COG3,VPS52,COG1
proton transmembrane transport	22.43	ATP6V0A2,ATP6V1B2,ATP6V1A,SLC16A1,COX7A2L
proton transmembrane transporter activity	22.26	ATP6V0A2,ATP6V1B2,ATP6V1A,SLC16A1,COX7A2L

GO Term	Fold Change	Genes
mitotic spindle midzone assembly	165.81	AURKB,PRC1,BIRC5
mitotic spindle elongation	165.81	AURKB,PRC1,BIRC5
spindle elongation	138.18	AURKB,PRC1,BIRC5
spindle midzone assembly	127.55	AURKB,PRC1,BIRC5
positive regulation of mitotic sister chromatid separation	103.63	ESPL1,AURKB,BIRC5
regulation of attachment of spindle microtubules to kinetochore	82.91	AURKB,ECT2,BIRC5
positive regulation of chromosome separation	61.41	ESPL1,AURKB,BIRC5
transcription corepressor binding	49.13	EZH2,ENO1,SUZ12,EED
PcG protein complex	46.06	EZH2,SUZ12,EED
mitotic cytokinesis	27.64	ESPL1,AURKB,ECT2,BIRC5
regulation of cytokinesis	24.56	AURKB,ECT2,PRC1,BIRC5
cytoskeleton-dependent cytokinesis	20.66	ESPL1,AURKB,ECT2,BIRC5
cytokinesis	20.28	ESPL1,AURKB,ECT2,BIRC5
transcription coregulator binding	20.10	EZH2,ENO1,SUZ12,EED
cellular response to radiation	16.55	AURKB,ECT2,ST20,BAK1,TLK2
mitotic cell cycle process	7.51	EZH2,ESPL1,AURKB,ECT2,PRC1,BIRC5,INTS3
regulation of cell cycle process	6.38	EZH2,ESPL1,AURKB,RBM14,ECT2,PRC1,BIRC5,INTS3
chromatin organization	6.26	EZH2,ENY2,MEAF6,RBM14,SUZ12,H1-5,EED,TLK2
protein-DNA complex organization	5.64	EZH2,ENY2,MEAF6,RBM14,SUZ12,H1-5,EED,TLK2