ras-in-3

RAS-IN-3 (compound 22) is a potent Ras inhibitor. ROCK-IN-12 is applicable for research in non-small cell lung cancer and colorectal cancer.

K-Ras-IN-3 (compound 3) is an effective inhibitor of GDP-KRAS G12V, exhibiting an IC50 value of 0.371 nM. It has potential for use in cancer research.

Pan-RAS-IN-3, a pan-Ras inhibitor, is applicable in the research of melanoma and acute myeloid leukemia.

Heterocyclic compounds as covalent inhibitors of G12C mutant K-Ras protein useful for treating cancers.K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.

Pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor suitable for cancer research [1].

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).

GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound comprising a ligand for the K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential for synthesizing PROTAC K-Ras Degrader-1, a potent degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

PROTAC K-Ras Degrader-3 is a PROTAC degrader targeting K-Ras, exhibiting a DC50 value of ≤ 1 nM against SW620 KRAS G12D and a GI50 value of ≤ 10 nM in inhibiting the growth of SW620 3D cells. It is used in cancer research.

YD-3 is a PAR4 antagonist that significantly inhibits thrombin-induced platelet aggregation in rabbits (IC(50)=28.3 microM). In addition, YD-3 suppresses thrombin-induced proliferation of vascular smooth muscle cells (VSMCs) and reduces neointimal thickening after balloon injury. Through Ras- and ERK1/2-mediated signaling pathways, YD-3 impedes thrombin-driven VSMC proliferation. When analyzed with Western blot, YD-3 primarily inhibits thrombin-induced expression of vascular endothelial growth factor receptor 2 (Flk-1) without affecting extracellular signal-regulated kinase 1/2 phosphorylation. YD-3 could potentially have value in elucidating the pathophysiology of thrombin-induced angiogenesis.

Clifutinib (Compound 9e) is an orally active, selective inhibitor of FMS-like tyrosine kinase 3 (FLT3-ITD) with an IC50 of 15.1 nM. It inhibits FLT3-ITD kinase activity and blocks downstream signaling pathways, including RAS/MAPK, PI3K/AKT, and JAK/STAT5. Clifutinib induces apoptosis in FLT3-ITD mutated acute myeloid leukemia (AML) cells and is a potential candidate for research in relapsed/refractory FLT3-ITD positive AML.

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1/2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB/HIF-2α axis[1][2][3].

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular signaling, vesicle fission and fusion, as well as mitochondrial division and fusion. It stimulates respiratory burst in neutrophils independent of diacylglycerol and activates monoacylglycerol acyltransferase, phospholipase C (PLC), Ras, and phosphatidylinositol 4-phosphate (PIP4) kinase in several cell lines. Phosphatidic acids (egg) is a mixture of phosphatidic acids isolated from chicken egg with fatty acids of variable chain lengths.

Magnolin reduces the renal oxidative stress, suppresses caspase-3 activity, and increases Bcl-2 expression in vivo and in vitro. Magnolin has anti-inflammatory and antioxidative effects.

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK . ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

Eicosapentaenoic Acid (EPA) sodium, an orally active omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA), demonstrates a unique ability to demethylate DNA, thereby facilitating the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). This compound also activates the RAS/ERK/C/EBPβ pathway by demethylating H-Ras intron 1 CpG island in U937 leukemia cells and promotes the relaxation of vascular smooth muscle cells, leading to vasodilation.

KRas G12R Inhibitor 1 (compound 3) is a selective covalent inhibitor targeting the KRas G12R mutation, leveraging the high nucleophilicity of mutant cysteines to bind irreversibly within the K-Ras Switch II region. This compound is utilized in cancer research [1].

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET. It impedes RET function, promoting autophagic breakdown of FLT3, and suppresses the PI3K and Ras/ERK pathways, contributing to its anti-leukemic effects. The compound's antitumor efficacy is demonstrated in both a mouse MV4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].

ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

Eicosapentaenoic Acid (Standard) is the standard substance of Eicosapentaenoic Acid, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.