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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
BCC4587 TAK-733 TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
BCC8037 AL 8697 AL 8697, a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM, 14-fold less potent in p38β MAPK (IC50=82 nM), exhibits anti-inflammatory activity.
BCC8080 KT 5720 KT5720 is a cell-permeable, potent, specific, reversible, ATP-competitive inhibitor of protein kinase A (PKA), with a Ki of 60 nM.
BCC7200 U0124
BCC4182 B-Raf inhibitor 1 B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
BCC2550 BIX 02188 BIX02188 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.
BCC2549 BIX 02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
BCC1771 MLN 2480 TAK-580 (MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.
BCC3998 PF-04880594 Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.
BCC8043 6-Bnz-cAMP sodium salt Cell permeable cAMP analog
BCC7236 SKF 86002 dihydrochloride
BCC7999 SR 3576
BCC4150 GDC-0623 GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
BCC1066 U0126-EtOH U0126-EtOH is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126-EtOH is an autophagy and mitophagy inhibitor.
BCC2013 Trametinib DMSO solvate Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
BCC1079 CEP-32496 Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
BCC4183 B-Raf inhibitor 1 dihydrochloride B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
BCC4393 Dabrafenib (GSK2118436) Dabrafenib is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
BCC1513 Dabrafenib Mesylate (GSK-2118436) Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.
BCC6511 BI-847325 BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
BCC6474 PF-03394197(Oclacitinib)
BCC1042 PKA inhibitor fragment (6-22) amide Potent protein kinase A inhibitor
BCC1953 Skepinone-L Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
BCC1468 CEP-32496 hydrochloride CEP-32496 Hcl is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.
BCC3639 TAK-632 TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
BCC2062 XMD8-92 XMD8-92 is a highly selective ERK5/BMK1 inhibitor with dissociation constant (Kd) value of 80 nM.
BCC2529 Pimasertib (AS-703026) Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
BCC7997 ML 786 dihydrochloride Potent Raf kinase inhibitor; orally bioavailable
BCC7006 KT 5823 KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
BCC4184 LGX818 Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
BCC6136 PF-3644022 PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
BCC2474 SP 600125 JNK inhibitor; prevents BMP9-induced osteogenic differentiation of MSCs,SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc.
BCC4997 H 89 2HCl H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
BCC5459 HG6-64-1 HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
BCC1437 B-Raf inhibitor TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
BCC4024 OTS514
BCC4025 OTS964 OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
BCC1672 JNK-IN-7 JNK-IN-7 is a potent JNK inhibitor with IC₅₀ of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
BCC1673 JNK-IN-8 JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.
BCC2061 XMD17-109 XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
BCC1458 CC-401 hydrochloride CC-401 hydrochloride is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM.
BCC6371 GDC-0994 Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
BCC3985 LY3009120 LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.
BCC8082 cAMPS-Rp, triethylammonium salt Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
BCC1093 SB202190 (FHPI) SB 202190 is a cell-permeable p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM.
BCC3663 SB 203580 SB 203580 (RWJ 64809) 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 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
BCC3969 PD 169316 PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.
BCC7982 CEP 1347
BCC1918 Salirasib Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
BCC1098 PD98059 PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
BCC8079 Dibutyryl-cAMP, sodium salt Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
BCC6521 DEL-22379 DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
BCC7538 Rp-8-Br-PET-cGMPS
BCC1923 SB 239063 SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
BCC4171 SB 242235 SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes.
BCC8087 PKI 14-22 amide, myristoylated Cell-permeable protein kinase A inhibitor
BCC3875 ZM336372 ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
BCC3966 VX-745 Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
BCC7428 PD 198306 Selective inhibitor of MEK1/2
BCC1112 PD184352 (CI-1040) CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
BCC4391 GW5074 GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
BCC7007 Anisomycin Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic isolated from Streptomyces griseolus.
BCC1937 SD-06 SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α.
BCC2535 BIRB 796 (Doramapimod) Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod (BIRB 796) has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod (BIRB 796) also inhibits B-Raf with an IC50 of 83 nM.
BCC3968 TAK-715 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
BCC7593 L-779,450 L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
BCC1123 SL-327 SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
BCC7731 SX 011
BCC8093 IQ 3
BCC5148 TCS JNK 5a TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
BCC7511 EO 1428
BCC1738 MEK inhibitor MEK inhibitor is a potent MEK inhibitor with antitumor potency.
BCC6464 AS601245 AS601245 is a cell-permeable JNK Inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively.
BCC7443 JX 401
BCC8090 BRD 7389 BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
BCC2539 PD318088 PD318088 is an allosteric MEK inhibitor.
BCC1277 PD0325901 PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.
BCC4269 CC-401 CC-401 is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM.
BCC7725 SU 3327 SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
BCC4392 SB590885 SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
BCC7274 CMPD-1 CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM.
BCC5777 JIP-1 (153-163)
BCC6225 HI TOPK 032 HI-TOPK-032 is a potent and specific TOPK inhibitor.
BCC6300 PD 334581
BCC5368 Losmapimod Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
BCC3672 PH-797804 PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
BCC3624 AZD6244 (Selumetinib) Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
BCC1148 MEK162 (ARRY-162, ARRY-438162) Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
BCC8085 c-JUN peptide
BCC8088 AEG 3482
BCC7568 XRP44X
BCC8078 8-Bromo-cAMP, sodium salt 8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
BCC8086 SL 0101-1 SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM. Shows proliferation inhibition in human breast cancer cell line MCF-7 and produces a cell cycle block in G1 phase.
BCC5773 10Z-Hymenialdisine
BCC8084 cGMP Dependent Kinase Inhibitor Peptide
BCC6178 Pluripotin Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
BCC1369 AS 602801 Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.
BCC2528 LY2228820 Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
BCC6084 AMG 548 AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
BCC3669 FR 180204 FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively.