Checkpoint Checkpoint

Cat.No.	Name	Information
M5137	BML-277	BML-277 is a high efficient Chk2 inhibitors, IC50 is 15 nM.
M2325	CHIR-124	CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM.
M1764	PF-477736	PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively.
M1665	AZD7762	AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.
M21501	Monalizumab	Monalizumab is a first-in-class immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab can be used in the study of head and neck squamous cell carcinoma (HNSCC).
M13622	Prexasertib	Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM.
M13621	GDC-0575 dihydrochloride	GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
M11418	SAR-020106	Sar-020106 is an ATP-competitive and selective CHK1 inhibitor with an IC50 of 13.3 nM. Sar-020106 has good selectivity to CHK2. Sar-020106 increased cell lethality of Gemcitabine and SN38 by 3.0 to 29 times in a p53-dependent manner in several colon cancer cell lines. Sar-020106 can enhance antitumor activity by selecting anticancer drugs.
M10476	GDC-0575 (ARRY-575)	GDC-0575 (ARRY-575, RG7741) is a potent and selective oral inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM.
M10129	CCT245737	CCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor, with IC50 values of 1.3 nM, 2440 nM and 30 nM for CHK1, CHK2 and G2 check point abrogation, respectively.
M9208	PD0166285	PD0166285 is a potent Wee1 inhibitor and Chk1 inhibitor with IC50s of 24 nM and 72 nM, respectively.
M9042	Prexasertib dihydrochloride	Prexasertib (LY2606368) is a substrate ATP competitively selective inhibitor of CHK1 and CHK2 with IC50 values of <1 nM and 8 nM against CHK1 and CHK2, respectively.
M6104	Ipilimumab	Ipilimumab (MDX-010, BMS-734016) is an immunomodulatory monoclonal antibody directed against the cell surface antigen CTLA-4 and also a type of immune checkpoint inhibitor.
M5156	CCT241533 hydrochloride	CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM.
M3686	AZD7762 hydrochloride	AZD7762 hydrochloride is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.
M2324	Rabusertib (LY2603618)	Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM.
M1996	SCH 900776	SCH 900776 (MK-8776) is a highly potent and functionally selective CHK1 inhibitor with IC50 of 3 nM.
M1676	BIBR1532	BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity.
M58411	PV-1019	PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits IR-induced apoptosis.
M55948	CCT241533 dihydrochloride	CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.

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