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Cell Cycle/Checkpoint Chk

Chk

Checkpoint kinase 1, commonly referred to as Chk1, is a serine/threonine-specific protein kinase that, in humans, is encoded by the CHEK1 gene. Chk1 coordinates the DNA damage response (DDR) and cell cycle checkpoint response. Activation of Chk1 results in the initiation of cell cycle checkpoints, cell cycle arrest, DNA repair and cell death to prevent damaged cells from progressing through the cell cycle.
Cat No. product name
T1830 BX795 BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respec...
T1837 BX912 BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PK...
T2033 BML-277 BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor.
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
T2517 MK-8776 CHK1 Inhibitor MK-8776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
T3700 SCH900776 S-isomer SCH900776 (S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM)...
T6028 PF-477736 PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
T6084 Rabusertib Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying t...
T6093 AZD7762 AZD7762, an effective and specific inhibitor of Chk1(IC50=5 nM), is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
T6156 S-Ruxolitinib Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
T6350 CHIR-124 CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against Cdc2 and CDK2/4.
T6931 PD0166285 PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
T4310 Prexasertib Prexasertib is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
T4327 Prexasertib dihydrochloride Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respe...
T7080 CCT245737 CCT245737 is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).
T7300 GDC-0575 GDC-0575 is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).
TN1458 Buddlejasaponin IV Buddlejasaponin IV has analgesic and anti-inflammatory effects, the inhibitions of the expressions of iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 by blocking NF-k...
T10325 ANI-7 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 g...
T14904 CCT244747 CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
T13148 CHK-IN-1 CHK-IN-1 is a CHK1 and CHK2 inhibitor, has anti-proliferative activities.
T10718 CCT241533 CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
T10718L CCT241533 hydrochloride CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
T10793 CHK1 inhibitor CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.
T10790 CHK1-IN-2 CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).
T10791 CHK1-IN-3 CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).
T10792 CHK1-IN-4 CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.
T16165 Myriocin Myriocin is a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia. Myriocin also is an effective inhibitor of serine-pa...
T16848 SB-218078 SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1...
T17223 VER-00158411 VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).
BX795
T1830CAS 702675-74-9
BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respec...
BX912
T1837CAS 702674-56-4
BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PK...
BML-277
T2033CAS 516480-79-8
BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor.
Baricitinib
T2485CAS 1187594-09-7
Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
MK-8776
T2517CAS 891494-63-6
CHK1 Inhibitor MK-8776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
SCH900776 S-isomer
T3700CAS 891494-64-7
SCH900776 (S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM)...
PF-477736
T6028CAS 952021-60-2
PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
Rabusertib
T6084CAS 911222-45-2
Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying t...
AZD7762
T6093CAS 860352-01-8
AZD7762, an effective and specific inhibitor of Chk1(IC50=5 nM), is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
S-Ruxolitinib
T6156CAS 941685-37-6
Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
CHIR-124
T6350CAS 405168-58-3
CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against Cdc2 and CDK2/4.
PD0166285
T6931CAS 185039-89-8
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
Prexasertib
T4310CAS 1234015-52-1
Prexasertib is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
Prexasertib dihydrochloride
T4327CAS 1234015-54-3
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respe...
CCT245737
T7080CAS 1489389-18-5
CCT245737 is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).
GDC-0575
T7300CAS 1196541-47-5
GDC-0575 is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).
Buddlejasaponin IV
TN1458CAS 139523-30-1
Buddlejasaponin IV has analgesic and anti-inflammatory effects, the inhibitions of the expressions of iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 by blocking NF-k...
ANI-7
T10325CAS 931417-26-4
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 g...
CCT244747
T14904CAS 1404095-34-6
CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
CHK-IN-1
T13148CAS 1278405-51-8
CHK-IN-1 is a CHK1 and CHK2 inhibitor, has anti-proliferative activities.
CCT241533
T10718CAS 1262849-73-9
CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
CCT241533 hydrochloride
T10718LCAS 1431697-96-9
CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
CHK1 inhibitor
T10793CAS 2097938-64-0
CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.
CHK1-IN-2
T10790CAS 912367-45-4
CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).
CHK1-IN-3
T10791CAS 2097252-39-4
CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).
CHK1-IN-4
T10792CAS 2120398-41-4
CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.
Myriocin
T16165CAS 35891-70-4
Myriocin is a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia. Myriocin also is an effective inhibitor of serine-pa...
SB-218078
T16848CAS 135897-06-2
SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1...
VER-00158411
T17223CAS 1174664-88-0
VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).