RO4987655 is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM)[1].

RGB-286638 free base is a CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively and less potent against cyclin H-CDK7 and cyclin D3-CDK6.

PD184161 is an orally-active MEK inhibitor with antitumor effects in HCC in vitro and in vivo that appear to correlate with suppression of MEK activity.

BIX-02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

OTS514 is a highly potent TOPK inhibitor with an IC50 value of 2.6 nM.

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor.

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.

OTS-964 is a TOPK (T-LAK cell originated protein kinase) inhibitor with IC50 value of 28 nM, which can specifically block cytokinesis, leading to apoptosis, in a broad range of cancer cells.

NQDI-1 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with IC50 of 3 μM and Ki of 500 nM.

GDC-0623 is a selective and ATP-uncompetitive MEK1 inhibitor with Ki value of 0.13 nM.

Trametinib is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.