Search Result
Results for "
Chk1 inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-131446
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-128766A
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-128601
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Checkpoint Kinase (Chk)
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Cardiovascular Disease
Cancer
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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 .
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- HY-139901
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- HY-177027
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-128766
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-171759
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-111369
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- HY-161383
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Checkpoint Kinase (Chk)
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Cancer
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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) .
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- HY-103367
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-171785
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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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 .
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- HY-162367
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FLT3
Checkpoint Kinase (Chk)
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Cancer
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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) .
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- HY-14720
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- HY-U00345
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- HY-18958
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- HY-112927
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- HY-10992
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- HY-10992A
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Checkpoint Kinase (Chk)
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Cancer
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AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
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- HY-124731
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- HY-112167A
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ARRY-575 dihydrochloride; RG7741 dihydrochloride
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Checkpoint Kinase (Chk)
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Cancer
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GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
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- HY-18958A
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- HY-107407
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Checkpoint Kinase (Chk)
CDK
PKC
Apoptosis
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Cancer
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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 .
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- HY-112167
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ARRY-575; RG7741
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Checkpoint Kinase (Chk)
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Cancer
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GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
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- HY-18942
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Checkpoint Kinase (Chk)
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Cancer
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VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively .
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- HY-148962
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Checkpoint Kinase (Chk)
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Cancer
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LY2880070 is an orally active CHK1 inhibitor, IC50 < 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents .
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- HY-18175
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Checkpoint Kinase (Chk)
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Cancer
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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.
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- HY-15532B
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MK-8776 S-isomer
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Drug Isomer
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Cancer
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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.
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- HY-40029
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- HY-10032
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PF 00477736
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Checkpoint Kinase (Chk)
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
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Cancer
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PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
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- HY-106009
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Checkpoint Kinase (Chk)
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Cancer
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VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC50 of 120 nM and a Ki of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.
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- HY-13263
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- HY-100195
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-19926
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RG-7602
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-13925
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Wee1
Apoptosis
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Cancer
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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 .
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- HY-13925A
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Wee1
Apoptosis
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Cancer
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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 .
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- HY-119699
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-18961
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- HY-136270
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VX-803; M4344; ATR inhibitor 2
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ATM/ATR
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Cancer
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Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki 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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- HY-112167B
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ARRY-575 hydrochloride; RG7741 hydrochloride
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Checkpoint Kinase (Chk)
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Inflammation/Immunology
Cancer
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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 .
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- HY-15532
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MK-8776
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-122198
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-155195
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FLT3
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Cancer
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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 .
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- HY-117857
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- HY-114302
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CCB02
1 Publications Verification
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-18174A
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LY2606368 dihydrochloride
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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. 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 .
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- HY-18174B
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LY2606368 Mesylate Hydrate; LY2940930
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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. 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 .
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- HY-18174C
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LY2606368 mesylate
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Checkpoint Kinase (Chk)
DNA/RNA Synthesis
Apoptosis
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Cancer
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Prexasertib mesylate (LY2606368 mesylate) 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. 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 .
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- HY-18174
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Prexasertib
Maximum Cited Publications
28 Publications Verification
LY2606368
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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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. 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 .
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- HY-112477
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Checkpoint Kinase (Chk)
Choline Kinase
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Cancer
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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 .
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- HY-15883
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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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 .
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- HY-18174E
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LY2606368 dimesylate
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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Prexasertib dimesylate (LY2606368 dimesylate) 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. 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 .
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- HY-15882
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Endogenous Metabolite
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Cancer
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GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
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- HY-16129A
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Calmodulin
MAP3K
MAPKAPK2 (MK2)
Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-16129
-
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Calmodulin
Checkpoint Kinase (Chk)
MAPKAPK2 (MK2)
MAP3K
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Cancer
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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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- HY-18174H
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LY2606368 lactate
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Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
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Cancer
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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 Ki 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 .
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- HY-13661
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UCN-01; KRX-0601
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Akt
PKC
CDK
Apoptosis
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Cancer
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7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
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- HY-172915
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MDM-2/p53
Apoptosis
Checkpoint Kinase (Chk)
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Cancer
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p53 Stabilizer 2 (Compound 17a16) is a p53 stabilizer. p53 Stabilizer 2 induces S-phase arrest and apoptosis in both p53-proficient and p53-deficient cancer cells. p53 Stabilizer 2 induces mitochondrial stress and activates two checkpoint pathways: NA-PKcs-dependent p53 stabilization and ATR-Chk1 axis activation. p53 Stabilizer 2 inhibits tumor growth in p53-deficient xenograft model .
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- HY-156470
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Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
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Cancer
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Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
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- HY-123597
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DDUG; NCI C04808
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Autophagy
Checkpoint Kinase (Chk)
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Cancer
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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- HY-161622
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Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-W341547
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Adrenergic Receptor
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Inflammation/Immunology
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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 .
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Cat. No. |
Product Name |
Type |
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- HY-40029
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(S)-(+)-3-Amino-1-boc-piperidine
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Biochemical Assay Reagents
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(S)-1-Boc-3-aminopiperidine is a key intermediate for the synthesis of various novel inhibitors, such as CHK1 inhibitors and PI3Kδ inhibitors .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-16129A
-
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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 .
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- HY-16129
-
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Calmodulin
Checkpoint Kinase (Chk)
MAPKAPK2 (MK2)
MAP3K
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Cancer
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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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