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Home > Inhibitors & Agonists > Ras-Raf-MAPK-ERK

Ras-Raf-MAPK-ERK

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Cat. No. Product Name Field of Application Chemical Structure
DC74349 NuP-3 Featured
NuP-3 is a potent, selective MAPK13 and MAPK14 inhibitor with IC50 of 7 and 14 nM, respectively.
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DC8473 Vacquinol-1 Featured
Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.
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DC10048 APS-2-79 Featured
APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
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DC44947 SM1-71 Featured
SM1-71 (Compound 5) is a highly effective TAK1 inhibitor, exhibiting a Ki value of 160 nM. Beyond its primary target, this compound demonstrates covalent inhibitory activity against a broad spectrum of kinases, including MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1, and RSK2. Due to its multi-kinase inhibitory profile, SM1-71 effectively suppresses the proliferation of various cancer cell lines, highlighting its potential as a promising therapeutic agent.
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DC72816 EB1 Featured
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation.
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DC1069 AZD6244 (Selumetinib,ARRY-142886) Featured
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.
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DC74339 HRX-0233 Featured
HRX-0233 (HRX0233) is a potent and selective inhibitor of MAP2K4 (MKK4), a kinase involved in the stress-activated protein kinase (SAPK) signaling pathway. MAP2K4 plays a role in regulating cellular responses to stress, apoptosis, and tumorigenesis. HRX-0233 has shown particular promise in KRAS-mutant cancers, where it exhibits synergistic effects with RAS inhibitors, making it a potential candidate for combination therapy in these difficult-to-treat cancers.
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DC7370 AZ-628 Featured
Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM For c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity For Raf kinases over a panel of 150 other kinases.
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DC8043 OTS514 Featured
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor. IC50:2.6nM
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DC74360 BC-DXI-32982 Featured
BC-DXI-32982 is a potent inhibitor of the interaction between DX2 and KRAS4B with a half-maximal inhibitory concentration (IC50) of 0.18 μM, showing little effect on the PRKACA-PRKAR2A interaction.
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DC43988 GW806742X hydrochloride
GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochlorid
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DC70371 DW0254 Featured
DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.
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DC74333 BAY-405 Featured
BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.
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DC70535 KAL-21404358 Featured
KAL-21404358 (KAL21404358) is a small-molecule, allosteric inhibitor of K-Ras(G12D), binds to K-Ras(G12D) P110 site with KD of 88 uM in MST assay; KAL-21404358 disrupts the K-RasG12D-B-Raf interaction using a NanoBiT split luciferase assay, and to impair the Raf-MEK-ERK and the PI3K-AKT signaling pathways. KAL-21404358 exhibited specificity for K-RasG12D over K-RasWT, H-RasWT, Rap1a, R-Ras and R-Ras2.
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DC74341 NFX-179 Featured
NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1).
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DC70730 Ras binder 2C07 Featured
Ras binder 2C07 is a switch-II binding ligand which binds Ras GDP and GTP states.
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DC74336 Darizmetinib Featured
Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.
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DC74365 RMC-4998 Featured
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.
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DC42419 Antineoplaston A10 Featured
Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
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DC70393 ETC-168 Featured
ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.ETC-168 acts as a MNK2-biased, dual-MNK inhibitor in cells.ETC-168 induced dose-dependent growth suppression and inhibited 50% of cell viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.ETC-168 effectively suppressed both p-4E and cell viability in MESSA cells, but not CGP57380 and eFT508.ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS cell, decreased expression of E2F1, FOXM1, and WEE1.Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.
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DC10496 PF06260933 Featured
PF 06260933 is a potent and selective MAP4K4 inhibitor (IC50 value 3.7 nM for MAP4K4 a.k.a. HGK or ZC1) with suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes, vascular inflammation and atherosclerosis.
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DC48953 Emprumapimod Featured
Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
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DC74347 NC-p38i NC-37 Featured
Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.
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DC7696 FMK Featured
Fmk is an irreversible ribosomal S6 kinase inhibitor 1/2 inhibitor.
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DC4177 Cobimetinib(GDC-0973; XL518) Featured
GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.
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DC74574 LY3537982 (KRAS G12C inhibitor 19)
LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.
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DC74369 SIJ1795
SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74368 SIJ1772
SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74367 SCH53239
SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein.
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DC74366 RSC-1255
RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.
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