MAPK Signaling
Targets for MAPK Signaling
- ERK(85)
- MEK1/2(74)
- NKCC(5)
- MNK(6)
- PKA(56)
- p38(103)
- Rac(2)
- Raf(76)
- RasGAP (Ras- P21)(1)
- JNK(66)
- cAMP(33)
- Protein Kinase G(2)
- RSK(33)
- Other(759)
- MAPKAPK(1)
- MKK(2)
- KLF(3)
- MAP3K(22)
- MAP4K(21)
- MAPKAPK2 (MK2)(9)
- Mixed Lineage Kinase(9)
Products for MAPK Signaling
- Cat.No. Product Name Information
- GC32900 CC-90003 CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
- GC10446 CC-930 A potent JNK inhibitor
- GC63441 CC-99677 CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM).
- GC19090 CCG215022 CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.
- GC19091 CCT196969 CCT196969, a pan-Raf inhibitor, inhibits B-Raf with an IC50 of 0.1 uM.
- GC40054 CCT241161 CCT241161 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively).
- GC61865 Cearoin Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK.
- GC12841 CEP 1347 JNK inhibitor
- GC16845 CEP-32496 CEP-32496 (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
- GC17860 CEP-32496 hydrochloride A potent inhibitor of B-Raf
- GC15525 cGMP Dependent Kinase Inhibitor Peptide cGMP Dependent Kinase Inhibitor Peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM.
- GC10666 CGP 57380 MNK1 inhibitor, specific and selective
- GC35674 Chicanine Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.
- GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
- GC12532 CHPG mGlu5 metabotropic glutamate receptor agonist
- GC17963 CHPG Sodium salt mGlu5 agonist
- GC47088 Cilostazol-d4 An internal standard for the quantification of cilostazol
- GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8
- GC38755 CKI-7 CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
- GC14693 CMK
- GC11180 CMPD-1 inhibitor of p38α-mediated MK2a phosphorylation
- GC10033 Cobimetinib A potent, orally available MEK1 inhibitor
- GC14337 Cobimetinib (R-enantiomer)
- GC17426 Cobimetinib (racemate)
- GC35719 Cobimetinib hemifumarate Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
- GC25289 CompK CompK (compound K), a potent and selective hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) small molecule inhibitor, significantly improves human T-cell functions, with enhanced T-cell receptor avidity to recognize tumor-associated antigens and tumor cytolytic activity by CD8+ T cells.
- GC46123 Comprehensive Kinase Screening Library For screening of a variety of kinase inhibitors
- GN10409 cor-nuside
- GN10481 Corynoxeine
- GC35734 Cot inhibitor-1 Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM.
- GC35735 Cot inhibitor-2 Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
- GC31525 CREBtide A PKA substrate
- GC43332 Cuspin-1 The Survival of Motor Neurons (SMN) protein participates in RNA splicing.
- GC50181 CW 008 PKA signaling activator; promotes osteogenesis from hMSCs
- GC43339 Cyclic di-AMP (sodium salt) Cyclic di-AMP (c-di-AMP) is a second messenger produced by bacteria but not by mammals.
-
GC43341
Cyclic GMP
Guanosine 3',5'-cyclic monophosphate (cyclic GMP or cGMP) is a second messenger that is biosynthesized from GTP by guanylate cyclases.
- GC30057 D-JNKI-1 (AM-111) D-JNKI-1 (AM-111) (AM-111) is a highly potent and cell-permeable peptide inhibitor of JNK.
- GC15187 Dabrafenib (GSK2118436) Dabrafenib (GSK2118436) (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
- GC12486 Dabrafenib Mesylate (GSK-2118436) A Raf kinase inhibitor
- GC47166 Dabrafenib-d9 An internal standard for the quantification of dabrafenib
- GN10336 Daphnetin
- GC14114 DB07268 A potent inhibitor of JNK1
- GC15477 DBM 1285 dihydrochloride p38 MAPK inhibitor
- GC16795 DCA 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.
- GC18666 Debromohymenialdisine Damaged DNA in humans is detected by sensor proteins that transmit a signal through checkpoint kinases (Chks) Chk1 and Chk2.
- GC35832 Dehydrocorydaline chloride An alkaloid with diverse biological activities
- GC16214 DEL-22379 inhibitor of the dimerization of ERK
- GC32254 Deltonin Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
- GC12824 Dibutyryl-cAMP, sodium salt Dibutyryl-cAMP, sodium salt salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator.
- GC38319 Dihydrocaffeic acid Dihydrocaffeic acid is a phenolic acid found in Gynura bicolor, reduces phosphorylation of MAPK p38 and prevent UVB-induced skin damage.
- GC31697 Dilmapimod (SB-681323) Dilmapimod (SB-681323) (SB-681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
- GC30913 DLK-IN-1 DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM.
- GC61466 DMU-212 DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.
- GC65298 DMX-5804 DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96).
- GC13244 DTP3 inhibitor of GADD45β/MKK7 complex
- GC38202 DTP3 TFA DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
- GC64496 EF24 EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
- GC10030 EHop-016 Rac1/Rac3 GTPase inhibitor,potent and specific
- GC43610 Enniatin A1 Enniatins are cyclohexadepsipeptides commonly isolated from fungi that are known to have antibiotic properties and to induce apoptosis in several cancer lines.
- GC17693 Enniatin B ionophore with some capacity to facilitate import of K+ and Na+ across membranes
- GC43611 Enniatin B1 Enniatins are cyclohexadepsipeptides commonly isolated from fungi and are known to have antibiotic properties.
- GC10403 EO 1428 p38α and p38β2 inhibitor
- GC43624 ERK Inhibitor ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM).
- GC33206 ERK-IN-1 ERK-IN-1 (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. ERK-IN-1 hydrochloride can also inhibit RAF.
- GC62229 ERK-IN-3 ERK-IN-3 is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
- GC63459 ERK-IN-3 benzenesulfonate ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
- GC65510 ERK1/2 inhibitor 1 ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
- GC60812 ERK1/2 inhibitor 2 ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
- GC67905 ERK1/2 inhibitor 7
- GC32796 ERK5-IN-1 An ERK5 inhibitor
- GC36002 ERK5-IN-2 ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.
- GP23419 ESAT6 Early Secretory Target Mycobacterium Tuberculosis Recombinant
- GC36006 Esculentoside H Thalidomide-O-PEG4-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
- GC38708 Esculin
- GC33033 ETC-206 ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
- GC61941 Eudesmin Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway.
- GC65329 EW-7195 EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
- GC67964 Exarafenib
- GC13869 Fasudil Calcium antagonist
- GC14289 Fasudil (HA-1077) HCl Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil (HA-1077) HCl is also a potent Ca2+ channel antagonist and vasodilator.
- GC40484 Ferulic Acid methyl ester Ferulic acid is a hydroxycinnamic acid that is abundant in plants and originally derived from giant fennel (F.
- GC25420 Fipexide hydrochloride Fipexide (hydrochloride) is a psychoactive drug of the piperazine class.
- GP23504 FLRT3 Human Fibronectin Leucine Rich Transmembrane Protein 3 Human Recombinant
- GC14125 FMK An inhibitor of RSK2
-
GC34197
FMK-MEA
A potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor
- GC32411 FR 167653 (FR 167653 sulfate) FR 167653 (FR 167653 sulfate) (FR 167653 (FR 167653 sulfate) sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity.
- GC31058 FR 167653 free base FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity.
-
GC10647
FR 180204
ERK inhibitor
- GC12970 Furosemide GABAA receptors antagonist
- GC36091 Furosemide sodium A loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter
- GC43734 Ganglioside GQ1b Mixture (sodium salt) Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit.
- GC14247 GDC-0623 MEK1 inhibitor, potent and ATP-uncompetitive
- GC10505 GDC-0879 B-Raf inhibitor,potent and selective
- GC12006 GDC-0994 GDC-0994 (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
- GN10307 Ginsenoside Re
- GC17255 Gliotoxin An immunosuppressive mycotoxin with diverse biological effects
- GC33123 GNE 220 GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
- GC34208 GNE 220 Hydrochloride GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
- GC19173 GNE-3511 GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.
- GC18257 GNE-495 GNE-495 is an orally bioavailable, potent, and selective MAP4K4 inhibitor (IC50 = 3.7 nM).