MAPK

KU004, a potent dual EGFR/HER2 inhibitor, exhibits anticancer properties. It inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR, and the downstream Akt and Erk pathways, primarily inducing apoptosis (Apoptosis) through the extrinsic pathway. Additionally, KU004 is a novel quinazoline derivative.

BI1701963 is an orally effective inhibitor that targets the SOS1 and KRAS interaction, specifically inhibiting the activation of KRAS by blocking its GTP loading. This compound is utilized in cancer research to explore potential therapeutic effects against KRAS-driven malignancies.

PF-05381941 is a selective and potent dual inhibitor of TAK1 and p38α that inhibits the kinase activity of TAK1 by binding to its active site.

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XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential,

PF-3644022 is a selective MK2 inhibitor, effective against TNFα (IC50: 5.2 nM, Ki: 3 nM), with anti-inflammatory properties. Also blocks MK3 and PRAK.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine

(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C.Cost-effective and quality-assured.

SD-169 (SD 169) is a selective and ATP competitive the MAP kinases p38α and p38β inhibitor.

DS03090629, an orally active MEK inhibitor, functions by competitively inhibiting MEK activity in the presence of ATP. This compound demonstrates strong binding affinity to both MEK and phosphorylated MEK, with dissociation constants (Kd) of 0.11 and 0.15 nM, respectively. It has shown efficacy in suppressing the proliferation of melanoma cell lines that overexpress BRAF mutations, achieving IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 is thus considered promising for anti-melanoma therapies.

Isochamaejasmine, isolated from S.

SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).

(R)-VX-11e is an isomer of VX-11e, a potent and selective ERK2 inhibitor with potential to inhibit tumor growth.

A-674563: Oral Akt inhibitor (Ki: 11 nM for Akt1), also targets PKA/Cdk2, with 10-1800x selectivity over other kinases.

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

MK2-IN-5, a pseudosubstrate of Mk2 with an inhibition constant (K_i) of 8 μM, selectively targets the protein interaction domain of the MAPK pathway and

Z16078526 promotes Ucp1, p38 MAPK, lipolysis, thermogenic genes, and mitochondrial activity in mouse brown adipocytes.

BI-2852: nanomolar affinity KRAS switch I/II pocket inhibitor; blocks signaling, halts KRAS mutant cell growth.

Ro-3201195 is a novel orally available p38 MAPK inhibitor with high selectivity.

Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and

(±)-Boehmenan inhibits PTP1B competitively (IC50=43.5µM), exhibits cytotoxicity in cancer cells, and affects mitochondria/EGFR in A549 NSCLC.

RWJ-67657 is a selective oral p38α/β MAPK inhibitor with IC50s of 1/11μM; inactive on p38γ/δ with cardioprotection.

PLK1/p38γ-IN-1 (compound 14) serves as a dual inhibitor targeting both PLK1 and p38γ kinases, effectively suppressing the proliferation of human hepatocellular

GW284543 (UNC10225170) is a selective inhibitor of MEK5 .

Kras4B G12D-IN-1 is an inhibitor of Kras4B G12D with anticancer activity.Kras4B G12D-IN-1 inhibits Kras protein expression.

R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.

FMK 是一种不可逆的 RSK2 抑制剂,能够共价修饰 RSK 的 C 末端区域。

XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).

Compound 2f (Antifungal Agent 46) is a potent antifungal that inhibits Ras signaling by targeting protein farnesyltransferase [1].

Tetrahydrocoptisine (Stylopine) quells inflammation, protects against ALI, guards the gut, and blocks key pro-inflammatory pathways.

ASK1-IN-1 inhibits apoptosis kinase 1, crucial in cell stress responses, with 21 nM IC50.

Ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid has anti-cancer activity, it induces apoptosis of human malignant cancer cells, it also inhibits hepatocellular

(E/Z)-Necrosulfonamide is a novel inhibitor of MLKL.

Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.

Cyclorasin 9A5 TFA is a cell-penetrating cyclic peptide consisting of 11 residues that inhibits the interaction between Ras and Raf proteins, with an IC50 of 120 nM.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.

AY 77: Potent, selective PAR2 agonist, favors Ca2+ (ec50=40nM) & ERK1/2 (ec50=2μM), boosts breast cancer cell migration.

Isoliquiritin apioside, from Glycyrrhizae radix, inhibits MMP9, MAPK, NF-κB, reduces cancer cell invasion, angiogenesis, and fights oxidative DNA damage.

APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization.

AM-001 is a non-competitive inhibitor of Epac1, preventing the activation of its downstream effector Rap1 in cultured cells. This compound is utilized in research related to cardiac diseases.

10-Methoxy-canthin-6-one (Mtx-C) acts as a DNA damage inducer that embeds into DNA, promoting cell cycle arrest at the G2/M phase. This process triggers myeloid differentiation in acute myeloid leukemia cells (AML) and leukemia stem cells (LSC). Differentiation in AML and LSC cells is characterized by increased expression of myeloperoxidase, CD15, CD11b, and CD14, along with the activation of p38 MAPK. 10-Methoxy-canthin-6-one is utilized in the study of leukemia.

TAK1-IN-3 is a novel ATP-competitive TAK1 inhibitor for the study of cancer.

Shizukaol B: anti-inflammatory, inhibits NO & JNK-AP-1 in LPS-microglia, low toxicity, anti-HIV, hampers monocyte-HUVEC adhesion.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical

AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).

AS601245 is an inhibitor of the c-Jun NH2-terminal kinase (JNK), with neuroprotective properties.

Cearoin suppresses inflammation, allergies, and NO production, and triggers autophagy and apoptosis in neuroblastomas via ROS.

NST-628 is a pan-RAF-MEK molecular glue that prevents RAF from phosphorylating and activating MEK. NST-628 inhibits the RAF-MEK signaling complex.

Broussonins A, new phytoalexins from mulberry, exhibit estrogenic effects, inhibit adipogenesis and reduce inflammatory iNOS in cells by modulating pathways.

Pan-RAS-IN-7 (Compound D101) is a broad-spectrum RAS inhibitor used in the synthesis of antibody-drug conjugates (ADCs). It is also applicable in cancer research.

KRAS inhibitor-34 (compound 27) is a KRAS inhibitor with an IC50 of 6.4 nM and is utilized in oncological research.

KRAS G12D inhibitor 14 is a potent inhibitor of KRAS G12D that binds KRAS G12D protein (Kd: 33 nM).

Dehydroglyasperin C: strong antioxidant, cancer preventive, neuroprotector, and combats chronic diseases.

ARS-1620 is a covalent inhibitor of K-RASG12C.

Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.

4,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the

IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.

SLV-2436 (SEL201-88) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).

GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) is a high kinase-selective

Ravoxertinib (GDC-0994) is an effective and orally available ERK1/2 inhibitor (IC50: 1.1/0.3 nM).

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM).

1588-A4 (ARS-1620 Intermediate) is an intermediate of ARS-1620 which is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.

Talmapimod (SCIO-469): Oral ATP-competitive p38α inhibitor, IC50 = 9 nM (p38α), 90 nM (p38β), >2000-fold selectivity over 20 kinases.

ERα degrader-2 is an estrogen receptor (SERD) degrader with anticancer activity that inhibits ERα for the prevention and treatment of HER-positive breast canc

MRTX-1257: selective, irreversible KRAS G12C inhibitor; IC50 of 900 pM; 31% bioavailable in mice; 77% target engagement.

Olomoucine hinders Cdk2, Cdc2, CDK5, ERK1, regulates the cell cycle, and fights melanoma; IC50s: 3-25 µM.

KRAS inhibitor-9 (DUN09716) hinders GTP-KRAS formation, with a Kd of 92 μM, causes G2/M arrest, and induces apoptosis in mutated NSC-LC cells.

KRAS G12C Inhibitor 60 (compound 23), a selective inhibitor targeting the Kras-G12C mutation, is utilized in the investigation of lung, colorectal, and

SCH772984 HCl selectively inhibits ERK1/2, acts like type I/II kinase inhibitors, and is potent at 4/1 nM IC50s in certain mutated tumor cells.

TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.

AZD4747 is an inhibitor of the mutant GTPase KRASG12C that hasial antitumor activity for the study of pancreatic and colorectal adenocarcinoma.

p38 Kinase inhibitor 8 (Compound CCLXXVIII) is an orally active inhibitor targeting p38β and JNK2α2, with IC50 values of 6.3 nM and 53.6 nM, respectively. It has demonstrated anti-inflammatory effects in a rat model of collagen-induced arthritis.

β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) is a promising agent for developing an improved strategy for radiotherapy against tumors.