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
- GC36652 MPT0B392 MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
- GC64292 MS432 MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
- GC65297 MW-150 MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
- GC34918 MW-150 dihydrochloride dihydrate MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
- GC49686 N-desmethyl Regorafenib N-oxide An active metabolite of regorafenib
- GC60262 N-Feruloyloctopamine N-Feruloyloctopamine is an antioxidant constituent. N-Feruloyloctopamine significantly decreases thephosphorylationlevels of Akt and p38MAPK.
- GC19260 NCB-0846 NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
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GC69543
NecroIr1
NecroIr1 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.
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GC69544
NecroIr2
NecroIr2 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.
- GC47771 NG 25 (hydrochloride hydrate) An inhibitor of MAP4K2 and TAK1
- GC13514 NG25 An inhibitor of MAP4K2 and TAK1
- GC17577 NQDI 1 A selective inhibitor of ASK1
- GC10069 NSC 23766 trihydrochloride Selective inhibitor of Rac1-GEF interaction.
- GC49186 O-Demethyl Apremilast An active metabolite of apremilast
- GC18951 Obscurolide A1 Obscurolide A1 is a natural butyrolactone isolated from S.
- GC48652 Olomoucine II A CDK inhibitor
- GC33857 Omtriptolide Omtriptolide (PG490-88) is a derivative prodrug of triptolide purified from the Chinese herb.
- GC50316 Org 48762-0 Selective p38α/β inhibitor; orally bioavailable
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GC12304
OTS514
TOPK inhibitor,highly potent
- GC16511 OTS964 OTS964 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 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
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GC69639
OVA-E1 peptide TFA
OVA-E1 peptide TFA is an antagonist mutant of SIINFEKL [OVA (257-264)]. OVA-E1 peptide activates the p38 and JNK cascades in both mutant and wild-type thymocytes.
- GC44530 p38 MAPK Inhibitor p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM).
- GC18602 p38 MAPK Inhibitor IV p38 MAPK Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively.
- GC33008 p38 MAPK-IN-1 p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM.
- GC30609 p38 MAPK-IN-2 p38 MAPK-IN-2 is an inhibitor of p38 kinase.
- GC62404 p38α inhibitor 2 p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6.
- GC31988 p38α inhibitor 1 p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
- GC30158 p38-α MAPK-IN-1 p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
- GN10752 Pachymic acid
- GC15814 Pamapimod (R-1503, Ro4402257) Pamapimod (R-1503, Ro4402257) (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively.
- GC36855 Paris saponin VII Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
- GC17737 PD 169316 P38 MAPK inhibitor
- GC15646 PD 184161 MEK1/2 inhibitor
- GC17964 PD 198306 MEK1/2 inhibitor
- GC17485 PD 334581 MEK1 inhibitor
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GC10397
PD0325901
A MEK inhibitor that sustains stem cell renewal
- GC63554 PD0325901-O-C2-dioxolane PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
- GC12989 PD184352 (CI-1040) PD184352 (CI-1040) (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
- GC10110 PD318088 Allosteric MEK1/2 inhibitor, non-ATP competitive
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GC12819
PD98059
PD98059 is a potent and selective MEK inhibitor with an IC50 of 2 μM.
- GC47931 PDE4B Inhibitor A PDE4B inhibitor
- GC44587 PDMP (hydrochloride) PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase.
- GC11857 Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) 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.
- GC50252 PF 06260933 dihydrochloride MAP4K4 (HGK) inhibitor; also inhibits MINK and TNIK
- GC14938 PF-03394197(Oclacitinib) Novel Janus kinase inhibitor
- GC15821 PF-04880594 RAF inhibitor
- GC63144 PF-05381941 PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
- GC31675 PF-06260933 PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
- GC14645 PF-3644022 Potent and Selective MK2 inhibitor
- GC10689 PF-4708671 PF-4708671, is a novel cell-permeable inhibitor of S6K1, specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM.
- GC10261 PH-797804 P38 MAP kinase inhibitor, potent and selective
- GC41635 Phosphodiesterase 4 Inhibitor Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.
- GC18050 Pimasertib (AS-703026) Pimasertib (AS-703026) (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
- GC10282 Piperlongumine An alkaloid with anticancer and antioxidant activities
- GC44653 PKA Inhibitor (5-24) PKA Inhibitor (5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM.
- GC48329 PKA Inhibitor (5-24) (trifluoroacetate salt) A synthetic peptide inhibitor of PKA
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GP10075
PKA inhibitor fragment (6-22) amide
A synthetic peptide inhibitor of PKA
- GC61512 PKA Inhibitor Fragment (6-22) amide TFA PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM.
- GC49265 PKI (14-22) amide (myristoylated) (trifluoroacetate salt) A PKA inhibitor
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GC69715
PKI (14-24)amide TFA
PKI (14-24)amide TFA is an effective inhibitor of PKA. In cell cytosol, PKI (14-24)amide strongly inhibits the activity of cyclic AMP-dependent protein kinase.
- GC12321 PKI 14-22 amide, myristoylated PKA inhibitor
- GC61849 PKI 14-22 amide,myristoylated TFA PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
- GC17407 Pluripotin dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP
- GC14732 PLX-4720 An orally-available inhibitor of the B-raf mutant B-RafV600E
- GC62206 PLX-4720-d7 PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an 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.
- GC10324 PLX7904 paradox-breaker RAF inhibitor, potent and selective
- GC64828 PLX7922 PLX7922, a RAF inhibitor, can bind with BRAFV600E. PLX7922 inhibits pERK in BRAFV600E cell lines, and activates pERK in mutant NRAS cell lines.
- GC32686 PLX8394
- GN10709 Polyphyllin A
- GC44673 PQ-10 PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; Ki = 4 nM).
- GC65479 PROTAC B-Raf degrader 1 PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
- GN10814 Quercitrin
- GC19304 R1487 Hydrochloride R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.
- GC61485 Raf inhibitor 2 Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
- GC37068 RAF mutant-IN-1 RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively.
- GC15818 RAF265 Multiple intracellular kinases inhibitor
- GC19307 RAF709 RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
- GC62504 RAS/RAS-RAF-IN-1 RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
- GC37071 Ravoxertinib hydrochloride Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
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GC16872
Refametinib
MEK 1/ MEK 2 inhibitor
- GC37516 Refametinib R enantiomer Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
- GC14606 Regorafenib hydrochloride A multi-kinase inhibitor
- GC14534 Regorafenib monohydrate A multi-kinase inhibitor
- GC40213 Regorafenib-13C-d3 Regorafenib-13C-d3 is intended for use as an internal standard for the quantification of regorafenib by GC- or LC-MS.
- GC18751 Reticulol Reticulol is an isocoumarin derivative produced by certain species of Streptomyces that inhibits cAMP phosphodiesterase (IC50 = 41 uM).
- GC37522 RGB-286638 A multi-kinase inhibitor
- GC37523 RGB-286638 free base A multi-kinase inhibitor
- GN10784 Rhoifolin
- GC50502 RI-STAD 2 AKAP disruptor; selectively binds PKA-RI with high affinity and blocks its interaction with AKAP; cell permeable
- GC62448 Rineterkib hydrochloride Rineterkib hydrochloride (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. Rineterkib hydrochloride can also inhibit RAF.
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GC69821
RLX-33
RLX-33 is an effective and selective relaxin family peptide 3 (RXFP3) antagonist with blood-brain barrier permeability. It also blocks the phosphorylation of ERK1/2 induced by relaxin 3, with IC50 values for RXFP3, ERK1, and ERK2 phosphorylation being 2.36 μM, 7.82 μM, and 13.86 μM respectively. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats. RLX-33 can be used for research on metabolic syndrome.
- GC50294 RMM 46 MSK/RSK family kinase inhibitor
- GC12141 RO4987655 MEK inhibitor
- GC12406 RO5126766(CH5126766) RO5126766(CH5126766) (CH5126766) 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).
- GC38609 Rotundic acid Rotundic acid, a triterpenoid obtained from I.
- GC15611 Rp-8-Br-PET-cGMPS cGMP-dependent protein kinase (PKG) inhibitor
- GC44852 Rp-8-bromo-Cyclic AMPS (sodium salt) Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP.
- GC44853 Rp-8-CPT-Cyclic AMP (sodium salt) Rp-8-CPT-Cyclic AMP (sodium salt), a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II.
- GC63176 Rp-cAMPS sodium salt Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 ?M and 4.5 ?M, respectively) antagonist.
- GC62269 RRD-251 RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.