MAPK Signaling

protein kinase C inhibitor

MK2 Inhibitor IV is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

DCA is a metabolic regulator in cancer cells' mitochondria with anticancer activity. DCA inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. DCA increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. DCA also works as NKCC inhibitor.

CEP-32496 (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

p38 MAPK inhibitor

AZD6244(Selumetinib) is an oral, small molecule, specific ATP non-competitive inhibitor of MEK1/2 proteins, with the IC 50 of 14.1 ± 0.79nM.

Gliotoxin, an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi, is a specific inhibitor of 20S proteasomal chymotrypsin activity with an IC 50 of 10μM.

ERK1 (p44) and ERK2 (p42) inhibitor

TCS JNK 6o (TCS JNK 6o) is a c-Jun N-terminal kinases (JNK-1, -2, and -3) inhibitor with Ki values of 2 nM, 4 nM, 52 nM, respectively, and has IC50 values of 45 nM and 160 nM for JNK-1 and -2, respectively.

A protein kinase G inhibitor

Sorafenib acts as a multi-kinase inhibitor, targeting Raf-1 and B-Raf with IC 50 values of 6 nM and 22 nM, respectively.

dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP

Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

MEK1 inhibitor

A selective inhibitor of ASK1

Anasthetic and class Ib antiarrhythmic agent

Guggulsterone is a plant sterol extracted from the resin of the plant Commiphora wightii. Guggulsterone can inhibit the growth of a wide variety of tumor cells and induce apoptosis through downregulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP, and survivin), modulation of cell cycle proteins (such as Cyclin D1 and c-Myc), activation of caspases, inhibition of Akt, and activation of JNK.

ionophore with some capacity to facilitate import of K+ and Na+ across membranes

allosteric inhibitor of oncogenic K-Ras(G12C)

Multi-AGC kinase inhibitor,ATP-competitive

p38 MAP kinase inhibitor

Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways. Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model. Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell.

dual inhibitor of MEK and Aurora kinases