MAPK
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Catalog No.
Product Name
Application
Product Information
Product Citation
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Aurora Kinase inhibitor
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition. -
CDK inhibitor
Voruciclib is a flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. -
PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
CDK inhibitor
Palbociclib is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.- Kana Nakatani, .et al. , Int J Hematol, 2020, Oct 17 PMID: 33068248
- Ryohei Ogata, .et al. , Breast Cancer, 2020, Aug 28 PMID: 32860163
- Kishino E, .et al. , Breast Cancer, 2019, Dec 10 PMID: 31823286
- Hidemasa Matsuo, .et al. , Blood Adv, 2018, Nov 13; 2(21): 2879-2889 PMID: 30381403
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
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CDK1 inhibitor
Ro 3306 is an ATP-competitive, potent cyclin-dependent kinase (cdk) 1 inhibitor (Ki values are 35 and 110 nM for cdk1/cyclin B1 and cdk1/cyclin A respectively).- Jianming Wang, .et al. , STAR Protoc, 2021, May 29;2(2):100570 PMID: 34136835
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
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G-quadruplex structures inhibitor
360A is a strong affinity and selectivity inhibitor of G-quadruplex structures. -
CDK inhibitor
AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM, less potent to CDK3 and little active to CDK7. -
Chk2 inhibitor
CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM. -
CDK9 inhibitor
CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor. -
ROCK inhibitor
H-1152 dihydrochloride, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. -
ROCK inhibitor
Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
ROCK inhibitor
Hydroxyfasudil hydrochloride, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
CDK inhibitor
NVP-LCQ195 is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. -
ROCK inhibitor
ROCK inhibitor is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively.- Delia Talpan, .et al. , Int J Mol Sci, 2023, Jan 11;24(2):1461 PMID: 36674976
- Nina Seidelmann, .et al. , J Cell Mol Med, 2021, Oct;25(20):9647-9659 PMID: 34486211
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ROCK2 Inhibitor
SLx-2119 is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM). -
CDK inhibitor
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor. IC50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. -
ROCK inhibitor
SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. -
KSR/Ras inhibitor
APS-2-79 HCl, small molecule that stabilizes the KSR (Kinase suppressor of Ras) inactive state and antagonizes oncogenic Ras signalling (IC50 value 120 nM against ATP-biotin probe-labelling of KSR2). -
CDC7 inhibitor
LY-3177833 is a potent and selective inhibitor of CDC7 (Cell Division Cycle 7-related Protein Kinase). -
CDK4/6 inhibitor
LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.- Shuso Takeda, .et al. , Fundam Toxicol Sci, 2021, 8(3):75-80
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GGTase I inhibitor
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
