Chk

Cat. No.

A11167

CAS No.

891494-63-6

SCH 900776 (MK-8776)

Synonyms: MK-8776

SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. It specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.

Cat. No.

A13684

CAS No.

1234015-52-1

Prexasertib (LY2606368)

Synonyms: LY-2606368

LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

Cat. No.

A11036

CAS No.

911222-45-2

Rabusertib (LY2603618, IC-83)

Synonyms: LY-2603618; IC-83

LY2603618 is a chk2 inhibitor that binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents.

Cat. No.

A13111

CAS No.

882531-87-5

R1530

R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.

Cat. No.

A15863

CAS No.

185039-89-8

PD0166285

PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.

Cat. No.

A10113

CAS No.

860352-01-8

AZD7762

AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor that drives checkpoint abrogation and potentiates DNA-targeted therapies.

Cat. No.

A11046

CAS No.

405168-58-3

CHIR-124

CHIR-124 is a novel and potent Chk1 inhibitor (IC50: 0.32 nM and 697 nM for Chk1 and Chk2 respectively).

Cat. No.

A11108

CAS No.

1262849-73-9

CCT241533

CCT241533 is a potent and selective Inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

Cat. No.

A11520

CAS No.

952021-60-2

PF 477736

Synonyms: PF-0044736

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively).

Cat. No.

A12703

CAS No.

891494-64-7

SCH900776 (S-isomer)

Synonyms: SCH-900776

SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

Cat. No.

A13142

CAS No.

912367-45-4

CHK1-IN-2

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.

Cat. No.

A13575

CAS No.

516480-79-8

BML-277

BML-277 (Chk2 Inhibitor II) is a Chk2 (checkpoint kinase 2) inhibitor.

Cat. No.

A14178

CAS No.

1200126-26-6

GNE-900

GNE-900 is an ATP-competitive, selective, and orally bioavailable ChK1 inhibitor.

Cat. No.

A15038

CAS No.

1431697-96-9

CCT241533 hydrochloride

CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.

Cat. No.

A15480

CAS No.

135897-06-2

SB 218078

SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively)

Cat. No.

A15550

CAS No.

1404095-34-6

CCT244747

CCT244747 is a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor with potential anticancer activity,

Cat. No.

A16811

CAS No.

1196541-47-5

GDC-0575 (ARRY-575, RG7741)

Synonyms: ARRY-575; RG7741; AK 687476

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.

Cat. No.

A17239

CAS No.

1489389-18-5

CCT245737

CCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor. CCT245737 showed CHK1 IC50 = 1.3 nM, CHK2 IC50 = 2440 nM, G2 check point abrogation IC50 = 30 nM. Mouse F (oral)=100%.

Cat. No.

A18443

CAS No.

2097252-39-4

CHK1-IN-3

CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.

Cat. No.

A19623

CAS No.

2097938-64-0

CHK1 inhibitor

Synonyms: GDC-0575 analog; GDC 0575

CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1.

Cat. No.

A21567

CAS No.

1657014-42-0

GDC-0575 dihydrochloride

Synonyms: ARRY-575 dihydrochloride; ARRY575; RG7741 dihydrochloride; RG 7741; GDC0575

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.

Cat. No.

A22129

CAS No.

203192-01-2

MN58b

MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis.

Cat. No.

A22156

CAS No.

1234015-54-3

Prexasertib 2HCl (LY2606368 dihydrochloride)

Synonyms: LY2606368 dihydrochloride

Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.

Cat. No.

A22371

CAS No.

1184843-57-9

SAR-020106

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1.

Cat. No.

A24191

CAS No.

2127107-15-5

Lasmotinib (PHI-101)

Synonyms: PHI-101

Lasmotinib (PHI-101) is a dual inhibitor of FLT3 and CHK2 with potent activity against FLT3 single activating mutations (ITD or TKD), as well as double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. It synergizes with Venetoclax or Azacytidine to enhance anti-leukemic effects and also demonstrates anticancer activity in ovarian and breast cancer models.