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Results for "

Chk1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Akt (1) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (15) ATM/ATR (1) Aurora Kinase (1) Autophagy (2) Biochemical Assay Reagents (1) c-Fms (1) c-Kit (1) Calmodulin (2) Casein Kinase (2) CDK (4) Checkpoint Kinase (Chk) (52) Choline Kinase (1) DNA/RNA Synthesis (2) Drug Intermediate (1) Drug Isomer (1) Early 2 Factor (E2F) (1) EGFR (1) Endogenous Metabolite (1) FGFR (1) FLT3 (4) MAP3K (2) MAPKAPK2 (MK2) (2) MDM-2/p53 (2) Microtubule/Tubulin (1) PDGFR (1) PI3K (1) Pim (1) PKC (2) RET (1) Src (1) Trk Receptor (1) VEGFR (1) Wee1 (3)
By Research Areas:	Cancer (58) Cardiovascular Disease (1) Inflammation/Immunology (3)

By Targets:

Adrenergic Receptor (1)

Akt (1)

Anaplastic lymphoma kinase (ALK) (1)

Apoptosis (15)

ATM/ATR (1)

Aurora Kinase (1)

Autophagy (2)

Biochemical Assay Reagents (1)

c-Fms (1)

c-Kit (1)

Calmodulin (2)

Casein Kinase (2)

CDK (4)

Checkpoint Kinase (Chk) (52)

Choline Kinase (1)

DNA/RNA Synthesis (2)

Drug Intermediate (1)

Drug Isomer (1)

Early 2 Factor (E2F) (1)

EGFR (1)

Endogenous Metabolite (1)

FGFR (1)

FLT3 (4)

MAP3K (2)

MAPKAPK2 (MK2) (2)

MDM-2/p53 (2)

Microtubule/Tubulin (1)

PDGFR (1)

PI3K (1)

Pim (1)

PKC (2)

RET (1)

Src (1)

Trk Receptor (1)

VEGFR (1)

Wee1 (3)

By Research Areas:

Cancer (58)

Cardiovascular Disease (1)

Inflammation/Immunology (3)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-131446

Chk1-IN-5 1 Publications Verification	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .

HY-128766A

CHK1-IN-4 hydrochloride	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity .

HY-128601

CHK1-IN-3	Checkpoint Kinase (Chk)	Cardiovascular Disease Cancer
CHK1-IN-3 is a potent and selective *CHK1* inhibitor with an IC₅₀ of 0.4 nM. CHK1-IN-3 effectively inhibits the growth of malignant hematopathy cell lines and displays low affinity for hERG (IC₅₀ > 40 μM). CHK1-IN-3 significantly suppresses the tumor growth in vivo. CHK1-IN-3 can be used for the study of hematologic malignancies .

HY-139901

Chk1-IN-6	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-6 is a potent, selective, and orally bioavailable *CHK1* inhibitor candidate.

HY-177027

CHK1-IN-13	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-13 (Compound 38) is a checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ of 10-50  nM. CHK1-IN-13 has anticancer activity, and can be used for the research of cancers, such as breast, ovarian and prostate cancer .

HY-128766

CHK1-IN-4	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity .

HY-171759

CHK1-IN-11	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-11 (Compound 1) is an orally active, checkpoint kinase 1 (CHK1) inhibitor. CHK1-IN-11 is useful for the study of cancers with oncogene amplification .

HY-111369

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

HY-161383

CHK1-IN-9	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-9 (compound 11) is an orally active *CHK1* inhibitor with an IC₅₀ value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .

HY-103367

CHK1-IN-7	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-7 (Compound 10c) is a potent human *CHK1* inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .

HY-171785

CHK1-IN-12	Checkpoint Kinase (Chk) Apoptosis	Cancer
CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC₅₀≤10 nM and cellular IC₅₀≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers .

HY-162367

FLT3/CHK1-IN-2	FLT3 Checkpoint Kinase (Chk)	Cancer
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and *CHK1, with IC₅₀s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1*-IN-2 can be used for research of acute myeloid leukemia (AML) .

HY-14720

Rabusertib 10+ Cited Publications LY2603618; IC-83	Checkpoint Kinase (Chk) Autophagy	Cancer
Rabusertib (LY2603618) is a potent and selective inhibitor of *Chk1* with an IC₅₀ of 7 nM.

HY-U00345

CHK-IN-1	Checkpoint Kinase (Chk)	Cancer
CHK-IN-1 is an inhibitor of *CHK1* and CHK2, with anti-proliferative activities.

HY-18958

CCT245737 2 Publications Verification SRA737	Checkpoint Kinase (Chk)	Cancer
CCT245737 (SRA737) is an orally active and seletive *Chk1* inhibitor, with an IC₅₀ of 1.3 nM.

HY-112927

MU380	Checkpoint Kinase (Chk)	Cancer
MU380 is a potent and selective *CHK1* inhibitor that induces apoptosis and has anticancer activity .

HY-10992

AZD-7762 20+ Cited Publications	Checkpoint Kinase (Chk)	Cancer
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

HY-10992A

AZD-7762 hydrochloride 20+ Cited Publications	Checkpoint Kinase (Chk)	Cancer
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for *Chk1*.

HY-124731

PD-321852	Checkpoint Kinase (Chk)	Cancer
PD-321852 is a *Chk1* inhibitor, with IC₅₀ of 5 nM. PD-321852 can be used in anti-cancer research .

HY-112167A

GDC-0575 dihydrochloride 5+ Cited Publications ARRY-575 dihydrochloride; RG7741 dihydrochloride	Checkpoint Kinase (Chk)	Cancer
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable *CHK1* inhibitor, with an IC₅₀ of 1.2 nM, and has antitumor activity.

HY-18958A

(S)-CCT245737 (S)-SRA737	Checkpoint Kinase (Chk)	Others
(S)-CCT245737 ((S)-SRA737) is a potent and selective oral inhibitor of checkpoint kinase 1 (CHK1).

HY-107407

SB-218078 5 Publications Verification	Checkpoint Kinase (Chk) CDK PKC Apoptosis	Cancer
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits *Chk1* phosphorylation of cdc25C with an IC₅₀ of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC₅₀ of 250 nM) and PKC (IC₅₀ of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .

HY-112167

GDC-0575 5+ Cited Publications ARRY-575; RG7741	Checkpoint Kinase (Chk)	Cancer
GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule *Chk1* inhibitor with an IC₅₀ of 1.2 nM.

HY-18942

VER-00158411	Checkpoint Kinase (Chk)	Cancer
VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC₅₀ values of 4.4 nM and 4.5 nM, respectively .

HY-148962

LY2880070	Checkpoint Kinase (Chk)	Cancer
LY2880070 is an orally active *CHK1* inhibitor, IC₅₀ ＜ 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents .

HY-18175

CCT244747 4 Publications Verification	Checkpoint Kinase (Chk)	Cancer
CCT244747 is a potent, orally bioavailable and highly selective *CHK1* inhibitor, with an IC₅₀ of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC₅₀ of 29 nM.

HY-15532B

SCH900776 (S-isomer) MK-8776 S-isomer	Drug Isomer	Cancer
SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC₅₀ of 3 nM.

HY-40029

(S)-1-Boc-3-aminopiperidine (S)-(+)-3-Amino-1-boc-piperidine	Biochemical Assay Reagents Drug Intermediate Checkpoint Kinase (Chk) PI3K	Others
(S)-1-Boc-3-aminopiperidine is a key intermediate for the synthesis of various novel inhibitors, such as *CHK1* inhibitors and PI3Kδ inhibitors .

HY-10032

PF 477736 5 Publications Verification PF 00477736	Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK	Cancer
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of *Chk1, with a K_i* of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .

HY-106009

VRX0466617	Checkpoint Kinase (Chk)	Cancer
VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC₅₀ of 120 nM and a K_i of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.

HY-13263

CHIR-124 3 Publications Verification	Checkpoint Kinase (Chk) FLT3 PDGFR Apoptosis	Cancer
CHIR-124 is a potent and selective *Chk1* inhibitor with IC₅₀ of 0.3 nM, and also potently targets PDGFR and FLT3 with IC₅₀s of 6.6 nM and 5.8 nM.

HY-100195

SAR-020106 1 Publications Verification	Checkpoint Kinase (Chk)	Cancer
SAR-020106 is an ATP-competitive, potent, and selective *CHK1* inhibitor with an IC₅₀ of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .

HY-19926

GDC-0425 RG-7602	Checkpoint Kinase (Chk)	Cancer
GDC-0425 (RG-7602) is an orally available, highly selective small molecule *ChK1* inhibitor. GDC-0425 can be used for the research of various malignancies .

HY-13925

PD0166285 5+ Cited Publications	Wee1 Apoptosis	Cancer
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 exhibits an IC₅₀ of 3.433 μM for Chk1 .

HY-13925A

PD0166285 dihydrochloride	Wee1 Apoptosis	Cancer
PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC₅₀ of 3.433 μM for Chk1 .

HY-119699

PV1115	Checkpoint Kinase (Chk)	Cancer
PV1115 is a potent and highly selective Chk2 inhibitor with an IC₅₀ of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2 .

HY-18961

PD 407824	Checkpoint Kinase (Chk) Wee1	Inflammation/Immunology Cancer
PD 407824 is a checkpoint kinase *Chk1* and WEE1 inhibitor with IC₅₀s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .

HY-136270

Gartisertib 2 Publications Verification VX-803; M4344; ATR inhibitor 2	ATM/ATR	Cancer
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a K_i of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC₅₀ of 8 nM. Antitumor activity .

HY-112167B

GDC0575 hydrochloride ARRY-575 hydrochloride; RG7741 hydrochloride	Checkpoint Kinase (Chk)	Inflammation/Immunology Cancer
GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active *Chk1* (IC₅₀=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research .

HY-15532

SCH900776 10+ Cited Publications MK-8776	Checkpoint Kinase (Chk)	Cancer
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC₅₀ of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .

HY-122198

ML367	Checkpoint Kinase (Chk)	Cancer
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .

HY-155195

FLT3/CHK1-IN-1	FLT3	Cancer
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC₅₀ value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .

HY-117857

MRT00033659	Casein Kinase Checkpoint Kinase (Chk) MDM-2/p53 Early 2 Factor (E2F)	Cancer
MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC₅₀=0.9 μM for CK1δ) and *CHK1* (IC₅₀=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation .

HY-114302

CCB02 1 Publications Verification	Microtubule/Tubulin	Cancer
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC₅₀ of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .

HY-18174A

Prexasertib dihydrochloride Maximum Cited Publications 28 Publications Verification LY2606368 dihydrochloride	Checkpoint Kinase (Chk) Apoptosis	Cancer
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .

HY-18174B

Prexasertib Mesylate Hydrate LY2606368 Mesylate Hydrate; LY2940930	Checkpoint Kinase (Chk) Apoptosis	Cancer
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .

HY-18174C

Prexasertib mesylate LY2606368 mesylate	Checkpoint Kinase (Chk) DNA/RNA Synthesis Apoptosis	Cancer
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib mesylate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .

HY-18174

Prexasertib Maximum Cited Publications 28 Publications Verification LY2606368	Checkpoint Kinase (Chk) Apoptosis	Cancer
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .

HY-112477

Chk2-IN-1	Checkpoint Kinase (Chk) Choline Kinase	Cancer
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC₅₀s of 13.5 nM and 220.4 nM for Chk2 and *Chk1*, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect .

HY-15883

GNE-900	Checkpoint Kinase (Chk) Apoptosis	Cancer
GNE-900 is a an ATP-competitive, selective, and orally active *ChK1* inhibitor with IC₅₀s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .

Cat. No.	Product Name	Target	Research Area

HY-16129A

CBP-501 acetate	Calmodulin MAP3K MAPKAPK2 (MK2) Checkpoint Kinase (Chk)	Cancer
CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser ²¹⁶-specific kinases, such as MAPKAP-K2, C-Tak1, *CHK1* and CHK2, with IC₅₀ values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer .

HY-16129

CBP-501	Calmodulin Checkpoint Kinase (Chk) MAPKAPK2 (MK2) MAP3K	Cancer
CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser ²¹⁶-specific kinases, such as MAPKAP-K2, C-Tak1, *CHK1* and CHK2, with IC₅₀ values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer .

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