MAPK

<p>KRpep-2d, a potent inhibitor of K-Ras, effectively suppresses the proliferation of cancer cells driven by K-Ras.</p>

<p>PROTAC SOS1 degrader-1: potent, DC50 98.4 nM, inhibits KRAS mutant cancer cells, low-toxic antitumor.</p>

<p>KRAS G12D inhibitor 17, a quinazoline-linked prolinamide, degrades mutant KRAS protein; a PROTAC.</p>

<p>CC-401 is a specific inhibitor of JNK (Ki: 25-50nM).</p>

<p>JNK-IN-14 is a potent inhibitor of JNK with IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3.</p>

<p>RM-018 inhibits active KRAS G12C &amp; G12C/Y96D, possibly beating resistance with unique traits.</p>

<p>Tagarafdeg (CFT1946) is a PROTAC degradator targeting mutant BRAF, capable of degrading BRAF V600E, G469A, G466V mutations, anti proliferation.</p>

<p>Rab8a GTPase-binding stapled peptide (Kd = 12.7 μM). Cell permeable; localizes to the endomembrane system.</p>

<p>GAGGVGKSAL, a wild-type KRAS G12D 10mer peptide, serves as an immunogenic neoantigen in cancer immunotherapy research [1].</p>

<p>KRAS inhibitor-24 (compound 115c), a pyrido-pyridine class KRAS inhibitor, exhibits potent activity against KRas G12V, KRas WT, and KRas G12R, with IC50 values all below 100 nM.</p>

<p>PD 198306: a MEK inhibitor with antihyperalgesic properties, reduces Streptozocin-boosted active ERK1.</p>

<p>PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM.</p>

<p>PROTAC SOS1 degrader-5 (compound 4) serves as an effective degrader of PROTAC SOS1, exhibiting a DC50 of 13 nM. It robustly suppresses the proliferation of NCI-H358 cells, with an IC50 value of 5 nM [1].</p>

<p>G12 (Ras5-17) TFA is a wild-type Ras peptide comprising amino acids 5-17 (KLVVVGAGGVGKS). It serves as a control in studies involving mutant Ras peptides, such as V12.</p>

<p>Anti-osteoporosis agent-8 (Compound 4aa) is a RANKL inhibitor, capable of preventing RANKL-induced osteoclastogenesis and osteoclast differentiation, with an IC50 of 2.41 μM. Furthermore, Anti-osteoporosis agent-8 has been shown to mitigate bone loss in an ovariectomized (OVX) mouse model.</p>

<p>WYE-687 is a selective mTOR inhibitor (IC50: 7 nM), over 100x more selective for mTOR than PI3Kα/γ, affecting mTORC1/pS6K and mTORC2/P-AKT(S473).</p>

<p>Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.</p>

<p>Pan-KRAS degrader 4 (compound 69) is a cereblon-based PROTAC KRAS degrader exhibiting anticancer activity with a DC50 value of less than 100 nM.</p>

<p>Ro-3201195 is a novel orally available p38 MAPK inhibitor with high selectivity.</p>

<p>MNK-IN-4 (compound D25) is a potent and selective MNK inhibitor used in treating acute spleen injury related to sepsis.</p>

<p>NUCC-0200808 (Compound 12g) is an MNK1 inhibitor with an IC50 of 42 nM. It reduces eIF4E phosphorylation and cell viability in AML cells and induces apoptosis. NUCC-0200808 shows potential for research in the field of leukemia.</p>

<p>The compound p38α inhibitor5 (compound 1) is a PROTAC-type ligand that targets p38 and is utilized in the synthesis of NR-11c.</p>

<p>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.</p>

<p>HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.</p>

<p>Pan-RAS-IN-5 (compound 7A) is a molecular glue that facilitates the formation of a ternary complex with cyclophilin A (CYPA) and RAS(ON) protein. This complex inhibits the binding of RAF downstream of RAS, demonstrating antitumor activity.</p>

<p>KRAS inhibitor-33 (compound 115a) is a pyrido[2,3-d]pyrimidine derivative that serves as an effective inhibitor of KRAS, exhibiting an IC50 value of ≤ 100nM.</p>

<p>QL-X-138 HCl is a BTK/MNK dual kinase inhibitor with anticancer activity and anti-dengue virus 2 activity that inhibits BTK, MNK1, and MNK2 kinases.</p>

<p>KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor with antitumor activity.</p>

<p>YN14 is a highly potent and selective KRASG12C proteolysis targeting chimera (PROTAC) capable of forming a stable KRASG12C: YN14: VHL ternary complex with low</p>

<p>BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.</p>

<p>PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2</p>

<p>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</p>

<p>Potent KRAS G12D inhibitor 15 targets cancer, potential for disease research. (WO2022042630A1, compound 243)</p>

<p>KRASG12C IN-2 (compound 17) is an orally active inhibitor of KRAS G12C, which effectively suppresses tumor growth in mice [1].</p>

<p>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.</p>

<p>JTP10-△-R9 TFA is a selective inhibitor of JNK2 peptide (IC50: 89 nM), exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.</p>

<p>Scio-323是一种可口服的 p38丝裂原活化蛋白（MAPK）激酶抑制剂。</p>

<p>KP-14 is a PROTAC specifically designed to target KRAS.</p>

<p>KS-58 is a derivative of KRpep-2d. It acts as an inhibitory peptide for K-Ras(G12D), selectively binding to K-Ras. KS-58 is capable of penetrating cells and interrupts the interaction between intracellular Ras and effector proteins. It inhibits the proliferation of tumor cells and exhibits antitumor activity.</p>

<p>MEK ligand-2, a ligand for the target protein for PROTAC (Ligand for Target Protein for PROTAC), functions as an inhibitor for both MEK1 and MEK2. This compound plays a crucial role in MS934, which is a VHL-recruiting MEK1/2 PROTAC degrader.</p>

<p>KRAS G12D inhibitor 6 is an efficacious compound that effectively inhibits KRAS G12D.</p>

<p>PROTAC K-Ras degrader-2 (compound 48) is a broad-spectrum KRAS mutant PROTAC degrader that demonstrates an IC50 of ≤200 nM for KRAS G12V/RAF1. Additionally, PROTAC K-Ras degrader-2 achieves a DC50 of ≤200 nM in degrading SW620 KRAS G12D and inhibits the growth of SW620 3D cells with an IC50 of ≤20 nM.</p>

<p>KRAS inhibitor-25 (compound 151a), a pyrido[2,3-d]pyrimidine derivative, effectively inhibits KRas G12V, KRas WT, and KRas G12R with IC50 values all below 100 nM.</p>

<p>PROTAC K-Ras Degrader-4 is a molecule designed to selectively degrade oncogenic K-Ras mutants, a novel strategy for cancer research.</p>

<p>Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib which is a selective MEK inhibitor.</p>

<p>PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].</p>

<p>OVA-E1 peptide TFA activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.</p>

<p>A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;</p>

<p>Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier and modulates ERK, NF-κB, and ACAT with an IC50 of 73 μM.</p>

<p>LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a</p>

<p>Tunlametinib is a MEK1/2 inhibitor (IC50=1.9 nM) for treating RAS/RAF-driven cancers.</p>

<p>Anti-ERK2 Antibody (5V598) is a Rabbit antibody targeting ERK2. Anti-ERK2 Antibody (5V598) can be used in ELISA.</p>

<p>Anti-ERK2 Antibody (4F551) is a Rabbit antibody targeting ERK2. Anti-ERK2 Antibody (4F551) can be used in ELISA,FCM.</p>

<p>Anti-ERK2 Antibody (9C922) is a Mouse antibody targeting ERK2. Anti-ERK2 Antibody (9C922) can be used in WB,ELISA.</p>

<p>TRPM4 inhibitor 8 is an inhibitor of Transient receptor potential melastatin 4(TRPM4) which contributes to viability, migration, cell cycle shift, and adhesion.</p>

<p>S6K1-IN-DG2(S6K1InhibitorDG2) is a potent p70S6K inhibitor with an IC50 value of less than 100 nM.</p>

<p>RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.</p>

<p>Enniatins B decreases the activation of ERK (p44/p42).</p>

<p>EM127: covalent SMYD3 inhibitor, KD 13μM, impedes ERK1/2, hinders SMYD3 gene regulation, long-term methyltransferase reduction, potential in cancer study.</p>

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

<p>JH295: potent, selective Nek2 inhibitor (IC50 = 770 nM), irreversibly targets Cys22, no effect on Cdk1, Aurora B, Plk1, or spindle mechanisms.</p>

<p>LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).</p>

<p>PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.</p>

<p>Gypenoside L inhibits autophagic flux and induces cell death in human esophageal cancer cells through endoplasm reticulum stress-mediated Ca2+ release.</p>

<p>TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.</p>

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

<p>A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and &gt;30-fold selective for Akt1 over PKC.</p>

<p>NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.</p>

<p>DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice</p>

<p>Irreversible K-Ras(G12C) inhibitor 6 fully modifies the protein at 10 μM after 24h in vitro.</p>

<p>PH-797804 is a pyridinone inhibitor of p38α (IC50: 26 nM, in a cell-free assay); 4-fold more selective versus p38β and does not inhibit JNK2.</p>

<p>methyl 5-(3,4-dimethoxyphenyl)isoxazole-3-carboxylate is a biochemical.</p>

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

<p>PF-06260933 Dihydrochloride, a MAP4K4 inhibitor, hinders HGK, Mink, Tnik (IC50s: 140, 8, 13 nM) and lessens mouse fasting hyperglycemia.</p>

<p>AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.</p>

<p>GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.</p>

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

<p>Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.</p>

<p>IQ3 inhibits JNK3 (Kd 66 nM), JNK1/2, NF-κB/AP1 in THP1-Blue cells (IC50 1.4 μM), and reduces TNF-α/IL-6 production.</p>

<p>Belvarafenib (HM95573) is a potent pan-RAF inhibitor with antitumor activity and inhibits B-RAF, B-RAFv600E, and C-RAF.Cost-effective and quality-assured.</p>

<p>Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.</p>

<p>Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.</p>

<p>Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently.</p>

<p>B-Raf IN 11 is a novel selective inhibitor.</p>

<p>Regorafenib HCl (BAY73-4506) is an oral inhibitor targeting angiogenic, stromal, and cancer kinases with strong antitumor effects.</p>

<p>LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.</p>

<p>LY-2584702 tosylate salt is a selective, ATP-competitive p70S6K inhibitor, used in trials studying the treatment of cancer.</p>

<p>Bohemine is a cyclin-dependent kinase inhibitor.</p>

<p>Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).</p>

<p>RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.</p>

<p>Maohuoside A promotes osteogenesis of rat mesenchymal stem cells via BMP and MAPK signaling pathways.</p>

<p>GNE-495 is a potent and specific MAP4K4 inhibitor (IC50: 3.7 nM).</p>

<p>MW-150 (MW01-18-150SRM) is a unique protein kinase inhibitor, is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.</p>

<p>AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM.</p>

<p>Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) is a potent and selective B-Raf inhibitor.</p>

<p>NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and</p>

<p>Necrosulfonamide ((E)-Necrosulfonamide) is a necroptosis inhibitor that targets MLKL and is selective. High-Quality, Low-Cost!</p>

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

<p>SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).</p>

<p>ASP2453 is a potent, selective and covalent inhibitor of KRAS G12C.</p>

<p>PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf.Cost-effective and quality-assured.</p>

<p>ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK.</p>

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

<p>BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).</p>

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