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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
91 Results for "
RAS/ERK
" in MedChemExpress (MCE) Product Catalog:
Products (91)
91 Results for "RAS/ERK" in MCE Product Catalog:
Cat. No.: HY-170550
KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein KRASG12C with an IC50 of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC50 of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC50 of 3.15 nM and 2.33 nM .
Cat. No.: HY-149539
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
Cat. No.: HY-119820
CAS No.: 135354-02-8
Synonyms: SR57746A free base
Target:
Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK
Research Areas:
Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-100388R
CAS No.: 1801747-42-1
Target:
Research Areas:
SHP099 (Standard) is the analytical standard of SHP099. This product is intended for research and analytical applications. SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth .
Cat. No.: HY-10966R
CAS No.: 405554-55-4
Target:
Research Areas:
SB-590885 (Standard) is the analytical standard of SB-590885 (HY-10966). This product is intended for research and analytical applications. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer .
Cat. No.: HY-107753R
CAS No.: 729605-21-4
Target:
Research Areas:
XRP44X (Standard) is the analytical standard of XRP44X (HY-107753). This product is intended for research and analytical applications. XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
Cat. No.: HY-50846R
CAS No.: 942183-80-4
Target:
Research Areas:
SCH772984 (Standard) is the analytical standard of SCH772984 (HY-50846). This product is intended for research and analytical applications. SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naive and MAPK inhibitor-resistant cells containing BRAF or RAS mutations .
Cat. No.: HY-175870A
CAS No.: 3024878-21-2
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
Cat. No.: HY-134505
CAS No.: 197787-17-0
Target:
Cat. No.: HY-101494R
CAS No.: 1951483-29-6
Synonyms: LY3214996 (Standard)
Target:
Research Areas:
Temuterkib (Standard) is the analytical standard of Temuterkib (HY-101494). This product is intended for research and analytical applications. Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
Cat. No.: HY-122465
CAS No.: 131123-73-4
Cat. No.: HY-182899
Research Areas:
DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma .
Cat. No.: HY-189075
CAS No.: 2843690-50-4
I-0436650 is an orally active SHP2 inhibitor with an IC50 of 4 nM and a Kd value of 0.3 nM. I-0436650 binds allosterically to the channel between the C-SH2, N-SH2 and PTP catalytic domains, locking the protein in an inactive closed conformation. I-0436650 potently inhibits ERK phosphorylation and suppresses MAPK pathway activity. I-0436650 exhibits antiproliferative activity in EGFR- and RAS-dependent cells. I-0436650 can be used in the research of RAS-driven cancers, EGFR-mutated cancers and RTK-driven cancers .
Cat. No.: HY-183674
CAS No.: 3096958-11-8
MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer .
Cat. No.: HY-N20754
DHA-free EPA oil is an EPA-enriched oil (HY-B0660) that does not contain DHA (HY-B2167). Eicosapentaenoic Acid (EPA) is an orally active ω-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid promotes DNA demethylation that re-expresses 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 H-RAS intron 1 CpG island. Eicosapentaenoic Acid promotes relaxation and vasodilation of vascular smooth muscle cells.
Cat. No.: HY-B0660S2
Synonyms: EPA-d10; Timnodonic acid-d10
Cat. No.: HY-156498R
CAS No.: 2765082-12-8
Research Areas:
RMC-7977 (Standard) is the analytical standard of RMC-7977 (HY-156498). This product is intended for research and analytical applications. RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
Cat. No.: HY-128393S2
Cat. No.: HY-111671R
CAS No.: 2245237-53-8
Synonyms: SOS1 activator 1 (Standard)
Research Areas:
VUBI1 (Standard) is the analytical standard of VUBI1 (HY-111671). This product is intended for research and analytical applications. VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer .
Cat. No.: HY-183365
SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
