checkpoint — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T6093	AZD-7762	AZD7762	Chk
	AZD-7762, an effective and specific inhibitor of Chk1（IC50=5 nM）, is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.		Chk
T5697	BMS-1166		PD-1/PD-L1
	BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor.		PD-1/PD-L1
T7080	CCT245737	SRA737	Chk
	CCT245737 (SRA737) is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).		Chk
T21331	SAR-020106		Chk
	SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.		Chk
T10565	BMS-1001 hydrochloride		PD-1/PD-L1
	BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activat...		PD-1/PD-L1
T2517	SCH900776	MK 8776,MK-8776	Chk , CDK
	SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.		Chk , CDK
T6350	CHIR-124	CHIR124,CHIR 124	Apoptosis , GSK-3 , FLT , Chk , PDGFR , Src
	CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.		Apoptosis , GSK-3 , FLT , Chk , PDGFR , Src
T6084	Rabusertib	LY2603618,IC-83	Chk , PDK , Autophagy
	Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cance...		Chk , PDK , Autophagy
T2033	BML-277	C 3742,Chk2 Inhibitor II,BML 277	Apoptosis , Chk
	BML-277 (C 3742) is a selective checkpoint kinase 2 (Chk2) inhibitor.		Apoptosis , Chk
T7300	GDC-0575	ARRY-575,RG7741	Chk
	GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).		Chk
T4327	Prexasertib dihydrochloride	LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368	Apoptosis , Chk , S6 Kinase
	Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.		Apoptosis , Chk , S6 Kinase
T4310	Prexasertib	LY2606368	Apoptosis , Chk
	Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.		Apoptosis , Chk
T6028	PF 477736	PF 00477736,PF-477736,PF-736,PF-00477736,PF477736	c-Fms , VEGFR , FGFR , FLT , c-RET , Chk , CDK , Src , Aurora Kinase
	PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
T2077	Adavosertib	AZD1775,MK-1775,Adavosertib (MK-1775)	Wee1
	Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.		Wee1
T9252	LY2880070		Chk
	LY2880070 is a new checkpoint kinase 1 (CHK1) inhibitor for cancer therapy.		Chk
T10792L	CHK1-IN-4 hydrochloride	CHK1-IN-4 hydrochloride（2120398-41-4 Free base）	Chk
	CHK1-IN-4 hydrochloride is a potent inhibitor of checkpoint kinase 1 (chk1). CHK1-IN-4 hydrochloride potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.		Chk
T10791	CHK1-IN-3		Chk
	CHK1-IN-3 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).		Chk
T10406	Tuvusertib	M1774,ATR inhibitor 1	Apoptosis , ATM/ATR , Others , Chk
	Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks...		Apoptosis , ATM/ATR , Others , Chk
T6931	PD0166285	PD-166285	Apoptosis , Wee1 , Chk
	PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.		Apoptosis , Wee1 , Chk
T14765	BOS-172722		Kinesin
	BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint(IC50 of 2 nM).		Kinesin