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MAPK Signaling

The mitogen-activated protein kinase (MAPK) family is a group of serine/threonine kinases that mediate intracellular signaling. The activation of MAPK involves a cascade consisting of MAPK kinase (also known as MAPKKK or MEKK) that activates MAPK/ERK (also known as MAPKK or MEK). This stimulates a phosphorylation-dependent increase in the activity of MAPK.

Products for MAPK Signaling

Cat.No. Product Name Information
BCC4293 SB 203580 hydrochloride SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
BCC3733 AZD8330 AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
BCC4122 VRT752271 Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
BCC1282 Trametinib (GSK1120212) Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
BCC5135 RO4987655 RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
BCC3730 AZ 628 AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
BCC8089 BI 78D3 BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM).
BCC7607 TCS JNK 6o JNK Inhibitor VIII (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.
BCC2051 VX-11e VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
BCC1459 CC-930 Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively.
BCC2482 GDC-0879 GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
BCC5615 SB 706504
BCC1269 Vemurafenib (PLX4032, RG7204) Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
BCC1436 BRAF inhibitor BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
BCC1280 PLX-4720 PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
BCC4276 Refametinib Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
BCC4055 Refametinib R enantiomer Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
BCC1519 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM.
BCC1491 Cobimetinib Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
BCC1493 Cobimetinib (R-enantiomer) Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
BCC1492 Cobimetinib (racemate) Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
BCC8081 cAMPS-Sp, triethylammonium salt
BCC1935 SCH772984 SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
BCC6509 Pexmetinib (ARRY-614) Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
BCC6374 RO5126766(CH5126766) Ro 5126766 is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
BCC5439 B-Raf IN 1 B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
BCN0119 VX-702