Talazoparib 0.006μM R06 exp299

Inhibits PARP1 and PARP2, blocks ssDNA break repair, selectively toxic to BRCA1/2 negative cancers

PubChem Name: Talazoparib
Synonyms: BMN-673; LT-673
CAS #: 1207456-01-6
PubChem CID: 135565082
IUPAC: (11S,12R)-7-fluoro-11-(4-fluorophenyl)-12-(2-methyl-1,2,4-triazol-3-yl)-2,3,10-triazatricyclo[7.3.1.05,13]trideca-1,5(13),6,8-tetraen-4-one
INCHI Name: InChI=1S/C19H14F2N6O/c1-27-18(22-8-23-27)15-16(9-2-4-10(20)5-3-9)24-13-7-11(21)6-12-14(13)17(15)25-26-19(12)28/h2-8,15-16,24H,1H3,(H,26,28)/t15-,16-/m1/s1
INCHI Key: HWGQMRYQVZSGDQ-HZPDHXFCSA-N
Molecular Weight: 380.4
Canonical SMILES: CN1C(=NC=N1)C2C(NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
Isomeric SMILES: CN1C(=NC=N1)[C@@H]2[C@H](NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
Molecular Formula: C19H14F2N6O

Characterization data not available.

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
5/16	Scores	View	View	View	View	View

GO Term	Fold Change	Genes
single-stranded DNA helicase activity	86.92	MCM9,RFC3,HELQ
double-strand break repair via nonhomologous end joining	60.70	XRCC1,RNF168,HELQ,SMARCAL1
recombinational repair	37.49	MCM9,H2AX,XRCC1,SPIDR,HELQ,SWSAP1,SFR1
site of DNA damage	35.41	H2AX,XRCC1,RIF1,RNF168,HELQ,SMARCAL1
double-strand break repair via homologous recombination	32.97	MCM9,H2AX,XRCC1,SPIDR,HELQ,SFR1
site of double-strand break	31.48	H2AX,RIF1,RNF168,SMARCAL1
positive regulation of DNA repair	31.35	H2AX,XRCC1,SPIDR,RIF1,RNF168,HELQ
double-strand break repair	28.54	MCM9,H2AX,XRCC1,SPIDR,RNF168,HELQ,SMARCAL1,SWSAP1,SFR1
DNA recombination	22.66	MCM9,H2AX,XRCC1,SPIDR,RNF168,HELQ,SWSAP1,SFR1
ATP-dependent activity, acting on DNA	22.17	MCM9,RFC3,HELQ,SMARCAL1
regulation of DNA recombination	20.08	SPIDR,CD28,RIF1,HELQ
regulation of DNA repair	18.93	H2AX,XRCC1,SPIDR,RIF1,RNF168,HELQ
positive regulation of DNA metabolic process	17.77	H2AX,XRCC1,RFC3,SPIDR,CD28,RIF1,RNF168,HELQ
DNA repair	14.89	MCM9,H2AX,XRCC1,RFC3,SPIDR,RIF1,RNF168,HELQ,SMARCAL1,SWSAP1,SFR1
catalytic activity, acting on DNA	13.45	MCM9,XRCC1,RFC3,HELQ,SMARCAL1
regulation of DNA metabolic process	10.06	H2AX,XRCC1,RFC3,SPIDR,CD28,RIF1,RNF168,HELQ
DNA damage response	9.81	MCM9,H2AX,XRCC1,RFC3,SPIDR,RIF1,RNF168,HELQ,SMARCAL1,SWSAP1,SFR1
DNA metabolic process	9.79	MCM9,H2AX,XRCC1,RFC3,SPIDR,RIF1,RNF168,HELQ,SMARCAL1,SWSAP1,SFR1
chromosome organization	8.65	MCM9,XRCC1,RFC3,RIF1,HELQ,SMARCAL1

GO Term	Fold Change	Genes
RecQ family helicase-topoisomerase III complex	552.40	RMI2,RMI1,BLM
resolution of recombination intermediates	331.44	RMI2,RMI1,BLM
small protein activating enzyme binding	276.20	UBA2,SAE1
regulation of protein sumoylation	75.33	UBA2,SAE1,UBE2I
protein sumoylation	64.99	PML,UBA2,SENP1,SAE1,UBE2I,SUMO2
PML body	31.57	PML,BLM,TOP3A,TP53,UBE2I,SUMO2
mitotic DNA damage checkpoint signaling	27.97	PML,BLM,TP53,MBTPS1
mitotic DNA integrity checkpoint signaling	26.62	PML,BLM,TP53,MBTPS1
peptidyl-lysine modification	20.21	PML,UBA2,SENP1,SAE1,UBE2I,SUMO2
double-strand break repair	13.74	RMI2,RMI1,BLM,TOP3A,TP53
nuclear body	7.50	RMI2,RMI1,PML,BLM,TOP3A,TP53,U2AF2,SLTM,UBE2I,THOC2,SUMO2