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Chk1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Checkpoint Kinase (Chk) (68) Adrenergic Receptor (1) Akt (1) Anaplastic lymphoma kinase (ALK) (1) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (18) ATM/ATR (4) Aurora Kinase (2) Autophagy (2) Bcl-2 Family (2) Biochemical Assay Reagents (1) c-Fms (2) c-Kit (1) c-Myc (1) Calmodulin (2) Casein Kinase (2) Caspase (2) CDK (6) Choline Kinase (1) DNA/RNA Synthesis (6) Drug Intermediate (1) Drug Isomer (1) Early 2 Factor (E2F) (1) EGFR (1) Endogenous Metabolite (1) ERK (1) FGFR (2) FLT3 (6) HDAC (1) Histone Demethylase (1) Isotope-Labeled Compounds (3) Ligands for Target Protein for PROTAC (1) MAP3K (2) MAPKAPK2 (MK2) (2) MDM-2/p53 (2) Microtubule/Tubulin (1) Microtubule‐associated serine/threonine kinase (MAST) (1) PARP (1) PD-1/PD-L1 (1) PDGFR (1) PI3K (1) Pim (1) PKC (1) PROTACs (2) Reactive Oxygen Species (ROS) (1) Reference Standards (1) RET (2) Src (2) STAT (1) TLK (1) Trk Receptor (1) VEGFR (2) Wee1 (6)
By Research Areas:	Cancer (78) Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (1)

By Targets:

Checkpoint Kinase (Chk) (68)

Adrenergic Receptor (1)

Akt (1)

Anaplastic lymphoma kinase (ALK) (1)

Antibody-Drug Conjugates (ADCs) (1)

Apoptosis (18)

ATM/ATR (4)

Aurora Kinase (2)

Autophagy (2)

Bcl-2 Family (2)

Biochemical Assay Reagents (1)

c-Fms (2)

c-Kit (1)

c-Myc (1)

Calmodulin (2)

Casein Kinase (2)

Caspase (2)

CDK (6)

Choline Kinase (1)

DNA/RNA Synthesis (6)

Drug Intermediate (1)

Drug Isomer (1)

Early 2 Factor (E2F) (1)

EGFR (1)

Endogenous Metabolite (1)

ERK (1)

FGFR (2)

FLT3 (6)

HDAC (1)

Histone Demethylase (1)

Isotope-Labeled Compounds (3)

Ligands for Target Protein for PROTAC (1)

MAP3K (2)

MAPKAPK2 (MK2) (2)

MDM-2/p53 (2)

Microtubule/Tubulin (1)

Microtubule‐associated serine/threonine kinase (MAST) (1)

PARP (1)

PD-1/PD-L1 (1)

PDGFR (1)

PI3K (1)

Pim (1)

PKC (1)

PROTACs (2)

Reactive Oxygen Species (ROS) (1)

Reference Standards (1)

RET (2)

Src (2)

STAT (1)

TLK (1)

Trk Receptor (1)

VEGFR (2)

Wee1 (6)

By Research Areas:

Cancer (78)

Cardiovascular Disease (2)

Inflammation/Immunology (3)

Metabolic Disease (1)

Neurological Disease (1)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Isotope-Labeled Compounds

Targets Recommended: Checkpoint Kinase (Chk)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18174

Prexasertib Maximum Cited Publications 33 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-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-136270

Gartisertib 5 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-14720

Rabusertib 20+ 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-18958

CCT245737 4 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-157941

ART0380	ATM/ATR Checkpoint Kinase (Chk) DNA/RNA Synthesis	Cancer
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC₅₀ of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent *Chk1* serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .

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-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-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-164734

Raludotatug Deruxtecan R-DXd; DS-6000	Antibody-Drug Conjugates (ADCs)	Cancer
Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC₅₀ of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, *Chk1* phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma .

HY-10032

PF 477736 4 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-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-18174A

Prexasertib dihydrochloride Maximum Cited Publications 33 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-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-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-18175

CCT244747 5 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-122198

ML367 1 Publications Verification	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-18174E

Prexasertib dimesylate Maximum Cited Publications 33 Publications Verification LY2606368 dimesylate	Checkpoint Kinase (Chk) Apoptosis	Cancer
Prexasertib dimesylate (LY2606368 dimesylate) 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 dimesylate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .

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-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-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-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-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-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-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-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 .

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 .

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-155798

CHK1-IN-8	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-8 (example 3-2) is a *Chk1* inhibitor with an IC₅₀ of <10 nM for human Chk1. CHK1-IN-8 can be used for the study of cancer .

HY-139901

Chk1-IN-6	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-6 is a selective and orally active *Chk1* inhibitor with an IC₅₀ of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .

HY-112927

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

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-W341547

3,4-Dihydro-6,7-isoquinolinediol	Adrenergic Receptor	Inflammation/Immunology
3,4-Dihydro-6,7-isoquinolinediol (compound 7) is a β2-AR agonist with an EC50 of 106.9 μM in CH-K1/GA1S cells. 3,4-Dihydro-6,7-isoquinolinediol can also inhibit the production of NO in mouse macrophage RAW 264.7 cells induced by lipopolysaccharide, showing anti-inflammatory activity .

HY-177551

CHK1-IN-14	Checkpoint Kinase (Chk)	Cancer
CHK1-IN-14 is a free base form of *CHK1* inhibitor. CHK1-IN-14 can be used in research on resistance to chemotherapy and radiotherapy .

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-178858

PROTAC FLT3/CHK1 Degrader-1	PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt	Cancer
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC *FLT3/CHK1* degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .

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-18174H

Prexasertib lactate LY2606368 lactate	Checkpoint Kinase (Chk) Apoptosis DNA/RNA Synthesis	Cancer
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate 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 lactate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .

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-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-159707

MCL1020	Checkpoint Kinase (Chk)	Cardiovascular Disease Cancer
MCL1020 is a *CHK1* inhibitor with an IC₅₀ of 1.61 μM. MCL1020 properly occupies the ATP pocket by interacting with a diverse range of the sites of CHK1 kinase. MCL1020 can be used for the study of hematologic malignancies .

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-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-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-156916

ST045945	Microtubule‐associated serine/threonine kinase (MAST)	Metabolic Disease
WAY-230563 (ST045945) is a serine/threonine kinase inhibitor that can block CHK1/CHK2-mediated cell cycle checkpoints. WAY-230563 can induce G2/M phase arrest and DNA damage in tumor cells .

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-161622

K1586	Checkpoint Kinase (Chk)	Cancer
K1586 is an amidine derivative that efficiently targets Chk1. K1586 enhances the degradation of Chk1 that sensitizes colorectal cancer cells to ionizing radiation. K1586 shows anticancer effects .

Cat. No.	Product Name	Target	Research Area

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 .

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 .

Cat. No.	Product Name	Chemical Structure

HY-18174S

Prexasertib-d4

Prexasertib-d₄ (LY2606368-d₄) is the deuterium labeled Prexasertib (HY-18174). 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-112167S

GDC-0575-d4
GDC-0575-d₄ (ARRY-575-d₄) is the deuterium labeled GDC-0575 (HY-112167). GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC₅₀ of 1.2 nM.

HY-136270S

Gartisertib-d8
Gartisertib-d₈ (VX-803-d₈) is the deuterium labeled Gartisertib (HY-136270). 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 .

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