MAPK

<p>RAS/RAS-RAF-IN-1: Potent RAS &amp; RAS-RAF inhibitor, KD 5-15μM for CYPA, antitumor properties.</p>

<p>JNK-IN-18 (compound 23b) is a potent inhibitor of JNK1, boasting an IC50 of 2 nM. It demonstrates superior efficacy when compared to its IC50 values of 125 nM for JNK2 and 98 nM for BRAF(V600E).</p>

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

<p>NEK7-IN-1 (Compound I-15) is an inhibitor of NIMA-related kinase 7 (NEK7) with an IC50 of less than 100 nM. It also effectively inhibits the release of IL-1β, exhibiting an IC50 of less than 50 nM.</p>

<p>RTIL 13 inhibits dynamin GTPase (IC50: 2.3 μM), targets its lipid binding domain, and suppresses endocytosis (IC50: 9.3 &amp; 7.1 μM).</p>

<p>SIAIS562055, a potent cereblon-based SOS1PROTAC, exhibits a dissociation constant (Kd) of 95.9 nM. It effectively degrades SOS1 and inhibits the downstream ERK pathway. SIAIS562055 disrupts the interaction between KRASG12C or KRASG12D and SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. This compound demonstrates strong anticancer activity.</p>

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

<p>Ras Inhibitory Peptide acetate, involved in cancer-related Ras signaling.</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>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.</p>

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

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

<p>Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control</p>

<p>Rineterkib hydrochloride (B) is an oral RAF/ERK1/2 inhibitor for MAPK-driven cancers, including KRAS/BRAF-mutant NSCLC and CRC.</p>

<p>14.3.3 protein antagonist, blocks binding to Raf-1/Bad/ASK1/exoenzyme S, competitive, no phosphorylation needed, KD ~80 nM.</p>

<p>KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.</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>D-JBD19 is a non-permeable peptide with neuroprotective effects.</p>

<p>KRas G12R inhibitor 1 targets mutant cysteines in K-Ras, binds irreversibly, and is used in cancer research.</p>

<p>KRas/SOS1 inhibitor; binds KRas pocket, Kd 106-176 nM; blocks nucleotide binding; cytotoxic to KRas-driven cancers; disrupts ERK-MAPK pathway; cell-permeable.</p>