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
- GC65949 GNE-9815 GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.
- GC38917 Gossypetin A flavonoid with diverse biological activities
- GC38791 GSK-25 GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM).
- GC60886 GSK356278 A selective PDE4 inhbitor
- GC43798 Guanylyl Imidodiphosphate (lithium salt) Guanylyl imidodiphosphate (Gpp(NH)p) lithium, a non-hydrolyzable GTP analogue, increases adenylate cyclase activity.
- GC17658 Guggulsterone Broad spectrum steroid receptor ligand
- GC36199 GW284543 GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
- GC11685 GW5074 C-Raf inhibitor,potent and selective
- GC36203 GW806742X GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM.
- GC61454 GW806742X hydrochloride GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
- GC63000 Gypenoside L Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum.
-
GC19396
H 89
A potent inhibitor of cyclic AMP-dependent protein kinase
- GC10074 H 89 2HCl H 89 2HCl 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.
- GC12799 H-8 (hydrochloride) H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor.
- GC43803 HA-1077 (hydrochloride) Fasudil (HA-1077; AT877) dihydrochloride 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. HA-1077 (hydrochloride) is also a potent Ca2+ channel antagonist and vasodilator.
- GN10248 Hesperitin
- GC36223 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.
-
GC12201
HI TOPK 032
T-LAK-cell-originated protein kinase (TOPK) inhibitor
- GC64035 Hirsutenone Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects.
- GN10664 Honokiol
- GC62514 HPK1-IN-3 HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM.
- GC63569 HPK1-IN-4 HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunotherapy tool compound.
- GC63006 HPK1-IN-7 HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
- GC63317 HPK1-IN-8 HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
- GC43885 Hypothemycin A resorcylic acid lactone polyketide
- GC25521 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.
- GC12674 IQ 3 Selective JNK3 inhibitor
- GC36327 IQ-1S free acid An inhibitor of NF-κB/AP-1
- GC39095 Isoliquiritin apioside Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.
- GN10023 Isorhamnetin
- GN10804 Isovitexin
- GC33844 Isovitexin (Saponaretin) A C-glycosylated flavone with diverse biological activities
- GC32209 ITX5061 ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
- GC36359 J30-8 J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2.
- GC65303 Jaspamycin Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei.
- GC13724 JIP-1 (153-163) Peptide inhibitor of c-Jun N-terminal kinase (JNK)
- GC15028 JNK-IN-7 A non-selective JNK inhibitor
- GC13841 JNK-IN-8 JNK-IN-8 is the first irreversible inhibitor of JNK, targeting JNK1, JNK2, and JNK3 with IC50 values of 4.7 nM, 18.7 nM, and 1 nM, respectively, in the A375 cell line.
- GC32983 Juglanin Juglanin, a natural occurring flavonoid, is a JNK acticator, with inflammation and anti-tumor activities.
- GC38804 JWG-071 JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology.
- GC13116 JX 401 p38α inhibitor
- GC11362 K 252a A protein kinase inhibitor
- GC17702 K-Ras(G12C) inhibitor 9 allosteric inhibitor of oncogenic K-Ras(G12C)
- GC13640 Kemptide substrate for cAMP-dependent protein kinase (PKA)
- GC36391 Kemptide Phospho-Ser5 Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
- GC33051 KO-947 An ERK inhibitor
-
GC14648
KT 5720
protein kinase A inhibitor, potent and selective
- GC17346 KT 5823 A protein kinase G inhibitor
- GC46015 KY 05009 A TNIK inhibitor
- GC15924 L-779,450 Raf kinase inhibitor
- GC44022 L-858,051 (hydrochloride) L-858,051 is a water-soluble analog of forskolin, a cell-permeant activator of adenylate cyclase.
- GC34275 L-JNKI-1 L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
- GC44085 L-Sulforaphene L-Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10-4 M. L-Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
- GC16576 LGX818 LGX818 (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
- GC36447 Licochalcone E Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
- GC17608 Lidocaine Anasthetic and class Ib antiarrhythmic agent
- GC33831 Lidocaine hydrochloride (Lignocaine hydrochloride) Lidocaine hydrochloride (Lignocaine hydrochloride) (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence.
- GC16039 LJH685 RSK (p90 ribosomal S6 kinase) inhibitor
-
GC16601
LJI308
pan-RSK inhibitor
- GC11157 LL-Z 1640-4 A signal-specific JNK/p38 pathway and TAK 1 inhibitor
- GC30770 LM22B-10 An activator of TrkB and TrkC
-
GC34650
Longdaysin
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of? 5.6 ?M, 8.8 ?M, 29 ?M, and 52 ?M, respectively.
- GC13717 Losmapimod p38 MAPK inhibitor, orally active
- GN10267 Loureirin B
-
GC19507
LUT-014
LUT014 is a topical B-Raf Inhibitor
- GC19228 LXH254 LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A.
- GC36505 LY-2584702 hydrochloride LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
- GC16835 LY2228820 LY2228820 (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively.
- GC12089 LY2584702 LY2584702 is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
- GC44095 LY2584702 (tosylate) LY2584702 (tosylate) is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
-
GC13980
LY3009120
LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and occupies both protomers in RAF dimers.
- GC19235 LY3214996 LY3214996 (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.
-
GC18241
Lysophosphatidylcholines
Lysophosphatidylcholines are produced by hydrolysis of the fatty acid of phosphatidylcholine at either the sn-1 or sn-2 position by phospholipase A2 (PLA2) or by lecithin-cholesterol acyltranferase (LCAT), which transfers the fatty acid to cholesterol.
- GC31735 Magnolin A lignan with anti-inflammatory and anticancer activities
- GC30545 Malantide Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
- GC63059 MAP4K4-IN-3 MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.
- GC64904 MAP855 MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
- GC30676 MAPK13-IN-1 MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM.
- GC11277 MEK inhibitor
- GC33388 MEK-IN-1 MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.
- GC12843 MEK162 (ARRY-162, ARRY-438162) MEK162 (ARRY-162, ARRY-438162) (MEK162) is an oral and selective MEK1/2 inhibitor. MEK162 (ARRY-162, ARRY-438162) (MEK162) inhibits MEK with an IC50 of 12 nM.
- GC33771 Metadoxine Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
- GC49241 Methyl Diethyldithiocarbamate An active metabolite of disulfiram
- GC36596 Methylnissolin Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM.
- GC16007 Methylthiouracil antithyroid preparation
- GC44211 MK2 Inhibitor III MK2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.
- GC16723 MK2 Inhibitor IV MK2 Inhibitor IV is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
- GC33142 MK2-IN-1 (MK2 Inhibitor) MK2-IN-1 (MK2 Inhibitor) is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
- GC61819 MK2-IN-3 MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM.
-
GC18156
MK8353
Selective and orally available ERK1/2 inhibitor
- GC62315 MKK7-COV-9 MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
- GC15296 ML 786 dihydrochloride Raf kinase inhibitor
- GC11307 ML-264 Krüppel-like factor 5 (KLF5) inhibitor
- GC49440 ML-9 A PKB/Akt inhibitor
- GC64634 MLK-IN-1 MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.
- GC63680 MLKL-IN-2 MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i).
- GC11649 MLN 2480 An oral pan-Raf kinase inhibitor
- GC64580 MMI-0100 MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2).
- GC48469 Moexipril-d5 An internal standard for the quantification of moexipril
- GC32789 Mogrol Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.