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Chk1-IN-5 is a potent checkpointkinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpointkinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity .
CHK1-IN-11 (Compound 1) is an orally active, checkpointkinase 1 (CHK1) inhibitor. CHK1-IN-11 is useful for the study of cancers with oncogene amplification .
CHK1-IN-4 (Compound 3) is a potent checkpointkinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity .
Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpointkinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs) .
CHK1-IN-13 (Compound 38) is a checkpointkinase 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 .
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpointkinase 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 .
CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpointkinase 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 .
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpointkinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .
SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpointkinase1 (Chk1) with IC50 of 3 nM.
NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpointkinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer .
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 checkpointkinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
PD 407824 is a checkpointkinaseChk1 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 .
Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpointkinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM) .
NSC 109555 is an ATP-competitive inhibitor of checkpointkinase 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.
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpointkinase 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 .
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpointkinase 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 .
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpointkinase 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 .
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpointkinase 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 .
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpointkinase 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 .
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpointkinase 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 .
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpointkinase 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 .
7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinaseAKT 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 checkpointkinasechk1, resulting in apoptosis .
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpointkinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpointKinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpointkinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs) .
Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpointkinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM) .
The CHEK2 protein is a serine/threonine protein kinase that critically coordinates checkpoint-mediated cell cycle arrest, DNA repair activation, and apoptosis in response to DNA double-strand breaks. Activated CHEK2 phosphorylates CDC25A, CDC25B, and CDC25C, inhibiting their phosphatase activities and preventing the CDK-cyclin complex from activating cell cycle progression. CHEK2 Protein, Human (sf9, GST) is the recombinant human-derived CHEK2 protein, expressed by Sf9 insect cells , with GST labeled tag.
CHEK2 is a serine/threonine protein kinase that coordinates cellular responses to DNA double-strand breaks by activating cell cycle arrest, DNA repair, and apoptosis. It phosphorylates effectors and inhibits CDC25A, CDC25B, and CDC25C, thereby enhancing CDK cyclin inhibition and cell cycle arrest. CHEK2 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived CHEK2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Chk1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 54 kDa, targeting to Chk1. It can be used for WB,ICC/IF,IP assays with tag free, in the background of Human, Mouse, Rat.
Phospho-Chk2 (Thr68) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 61 kDa, targeting to Phospho-Chk2 (Thr68). It can be used for WB,ICC/IF,IHC-P assays with tag free, in the background of Human, Mouse, Rat.
Chk1 Antibody (YA5995) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Chk1. It can be applicated for WB, ICC/IF, IP, ELISA assays, in the background of human, mouse, rat.
Chk2 Antibody (YA6186) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Chk2. It can be applicated for WB, IHC-P, ICC/IF, IP, ELISA assays, in the background of human, mouse, rat.
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