MAPK

<p>JNK-IN-13 is a JNK inhibitor that inhibits JNK3 and JNK2 and can be used in the study of diabetes, inflammation, and neurological disorders.</p>

<p>GW806742X inhibits MLKL with Kd 9.3 μM, preventing necroptosis; also targets VEGFR2.</p>

<p>Tanzisertib (CC-930) (CC-930) is a potent inhibitor of JNK1/2/3 with IC50s of 61/7/6 nM, respectively, with potential antifibrotic activity.</p>

<p>XL-281: potent oral RAF kinase inhibitor, effective on wild-type and mutants, reduces tumor growth and cell proliferation, increases apoptosis.</p>

<p>Regorafénib N-oxyde M2 is an active metabolite of Regorafenib.</p>

<p>K-Ras G12C-IN-4 是一种 KRAS G12C 共价抑制剂。</p>

<p>INH154 is a potent Nek2 and Hec1 binding (INH) inhibitor with IC50s of 120 nM in MB468 cells and 200 nM in Hela cells for INH.</p>

<p>RMC-6236 is a potent RAS(ON)MULTI inhibitor with broad-spectrum inhibitory activity against RAS-GTP.Cost-effective and quality-assured.</p>

<p>HI-TOPK-032 is an effective and specific inhibitor of TOPK.</p>

<p>ERK5-IN-6 is an ERK5 kinase inhibitor with antiproliferative, anticonvulsant, and antitumor activity for the study of central nervous system related diseases.</p>

<p>AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).</p>

<p>ARS-1630 is a mutant K-ras G12C inhibitor. It is a less active enantiomer of ARS-1620.</p>

<p>MAP4K4-IN-3 (Compound 17) may be a viable target for antidiabetic agents, a serine/threonine protein kinase.</p>

<p>MK2-IN-3 hydrate (MK-2 Inhibitor III) is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)</p>

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

<p>BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.</p>

<p>Divarasib (GDC-6036), an investigational KRAS G12C inhibitor for solid tumors, has an IC50 of &lt;0.01 μM.</p>

<p>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.</p>

<p>(R)-Ketorolac ((+)-Ketorolac) is the R-enantiomer of Ketorolac, with potent analgesic activity.</p>

<p>Dilmapimod (SB-681323) is a potent inhibitor of p38 MAPK ,it potentially suppresses inflammation in chronic obstructive pulmonary disease.</p>

<p>ERK5-IN-5 is extracellular signal-regulated kinase 5 (ERK5) inhibitor with anticancer activity anticonvulsant activity inhibits A549 cell proliferation.</p>

<p>Pepinh-TRIF TFA is a 30 aa peptide associated with the immune system that blocks TRIF signaling by interfering with TLR-TRIF interaction (TLR-TRIF interaction</p>

<p>B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research.</p>

<p>Cephradine (Anspor) is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.</p>

<p>LUT014 is a B-Raf inhibitor (IC50: 11.7 nM) and developed to decrease dose-limiting acneiform lesions associated with EGFR Inhibitors treatment.</p>

<p>Azelnidipine (UR-12592) is a dihydropyridine used as calcium channel blocker.</p>

<p>CC-90003 is a selective inhibitor of ERK 1/2. It has antitumor activity.</p>

<p>ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).</p>

<p>Methylthiouracil (NSC-193526) is a thiourea antithyroid agent that inhibits the synthesis of thyroid hormone, and it is used to treat hyperthyroidism.</p>

<p>SU3327 (halicin) is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 μM).</p>

<p>MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.</p>

<p>KRAS G12C inhibitor 19 is a potent KRAS G12C inhibitor that shows anti-tumor activity in cellular assays, and the family inhibits tumor growth.</p>

<p>KRAS Inhibitor-38 (Example 18) is a potent inhibitor capable of effectively suppressing the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo.</p>

<p>NecroX-2 is a cell-permeable necrosis inhibitor with antioxidant properties. NecroX-2 selectively suppresses necrotic cell death triggered by oxidative stress. NecroX-2 does not confer protection against apoptosis induced by staurosporine or etoposide but shows protective effects under conditions such as cold shock, hypoxia, and oxidative stress in vitro.</p>

<p>JNK3 inhibitor-8: potent, selective, oral, BBB-penetrating, IC50: JNK3=21 nM, JNK2=2203 nM, JNK1&gt;10,000 nM; potential in Alzheimer's research.</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>Peptide (45-60) blocks Rac1 binding with TrioN, GEF-H1, Tiam1 GEFs.</p>

<p>Negative control for LC 2.</p>

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

<p>KRAS G12C inhibitor 18 is a potent, orally active compound that inhibits KRAS G12C and exhibits anti-tumor activities.</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>HPK1-IN-8 is an allosteric, inactive, conformation-selective triazolopyrimidine ketone HPK1 inhibitor.</p>

<p>KRAS G12C inhibitor 69 (Compound K09) is an inhibitor of the mutant RAS protein KRAS G12C with an IC50 of 4.36 nM. In the cell lines NCI-H358 and MIA-PACA-2, it suppresses ERK phosphorylation with IC50 values of 12 nM and 7 nM, respectively. Additionally, KRAS G12C inhibitor 69 hinders the proliferation of NCI-H358 and MIA-PACA-2 cancer cells, with IC50 values of 3.15 nM and 2.33 nM, respectively.</p>

<p>MC 976 is a derivative of Vitamin D3.</p>

<p>SS47 is a PROTAC that degrades immunosuppressive HPK1 via proteasome; boosts BCMA CAR-T cell cancer therapy.</p>

<p>12-oxo PDA boosts alkaloid production in E. californica, enhances B. dioica tendril curls, and blocks JA-induced cell death in A. fru mutants.</p>

<p>KG5 inhibits PDGFRβ, B-Raf, FLT3, KIT, c-Raf; has anticancer and antiangiogenic effects; Kd: 520 nM (PDGFRβ), 300 nM (PDGFRα).</p>

<p>MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.</p>

<p>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.</p>

<p>ADT-007 is a pan-RAS inhibitor with potent anticancer activity.</p>