GW284543, also known as UNC10225170, is a 4-anilinoquin(az)oline chemotype that selectively inhibits MEK5.

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway.

ASK1 Inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1). It is selective for ASK1 over ASK2 as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF. It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner.

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.

PD 198306是一种选择性 MAPK/ERK 激酶 (MEK) 抑制剂，能够显著降低Streptozocin诱导的ERK1/2活性升高，具有抗痛觉过敏作用，并可用于与MAPK/ERK相关疾病的研究。

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 (GSK1120212；JTP-74057) 是一种口服活性的 MEK 抑制剂，抑制 MEK1 和 MEK2 的 IC50 值约为 2 nM。Trametinib 激活自噬并诱导细胞凋亡。

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

Zapnometinib is a MEK inhibitor, with an IC50 of 5.7 nM.

Cobimetinib (GDC-0973，RG7420) 是一种强效、选择性、口服 MEK1 抑制剂，对 MEK1 的 IC50 为 4.2 nM。

SL327 is a cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK-1 and MEK-2 (IC50 = 0.18 and 0.22 μM respectively).

Selonsertib (GS-4997) 是一种口服可用和选择性的凋亡信号调节激酶 1 (ASK1) 抑制剂，pIC50 为 8.3，已被研究作为治疗糖尿病肾病和肾纤维化的潜在药物。

Selumetinib(AZD6244) 是一种选择性、非ATP竞争性口服MEK1/2抑制剂，对MEK1的IC50为14 nM，并抑制ERK1/2的磷酸化。