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Results for "

RAF/MEK

" in MedChemExpress (MCE) Product Catalog:

By Targets:	MEK (12) Raf (10) Antibiotic (1) Apoptosis (2) Autophagy (1) Bacterial (1) Bcl-2 Family (1) Beta-secretase (2) c-Fms (1) CDK (1) Cholinesterase (ChE) (2) Cyclin G-associated Kinase (GAK) (1) Endogenous Metabolite (1) ERK (3) Ferroptosis (1) Glutathione S-transferase (1) HBV (1) HCV (1) HDAC (1) HIV (1) HSP (1) Interleukin Related (1) JNK (1) Microtubule/Tubulin (1) Molecular Glues (1) mTOR (1) NF-κB (1) P-glycoprotein (1) p38 MAPK (1) Phosphatase (1) Ras (3) Reactive Oxygen Species (ROS) (2) SHP2 (1) Smo (1) Tie (1) TNF Receptor (1) VEGFR (1)
By Research Areas:	Cancer (18) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (2)

By Targets:

MEK (12)

Raf (10)

Antibiotic (1)

Apoptosis (2)

Autophagy (1)

Bacterial (1)

Bcl-2 Family (1)

Beta-secretase (2)

c-Fms (1)

CDK (1)

Cholinesterase (ChE) (2)

Cyclin G-associated Kinase (GAK) (1)

Endogenous Metabolite (1)

ERK (3)

Ferroptosis (1)

Glutathione S-transferase (1)

HBV (1)

HCV (1)

HDAC (1)

HIV (1)

HSP (1)

Interleukin Related (1)

JNK (1)

Microtubule/Tubulin (1)

Molecular Glues (1)

mTOR (1)

NF-κB (1)

P-glycoprotein (1)

p38 MAPK (1)

Phosphatase (1)

Ras (3)

Reactive Oxygen Species (ROS) (2)

SHP2 (1)

Smo (1)

Tie (1)

TNF Receptor (1)

VEGFR (1)

By Research Areas:

Cancer (18)

Cardiovascular Disease (1)

Infection (3)

Inflammation/Immunology (1)

Metabolic Disease (3)

Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Targets Recommended: Raf MEK ASK1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153181

Trametiglue	MEK	Cancer
Trametiglue, a derivative of Trametinib (HY-10999), targets both *KSR-MEK* and *RAF-MEK* with unprecedented potency and selectivity via unique interfacial binding interactions .

HY-14947

Balamapimod MKI 833	MEK	Cancer
Balamapimod (MKI 833) is a reversible *Ras/Raf/MEK* inhibitor with potential anti-tumor activity.

HY-18652

Avutometinib 3 Publications Verification Ro 5126766; CH5126766	MEK Raf	Cancer
Avutometinib (Ro 5126766) is a first-in-class dual *MEK/RAF* inhibitor that allosterically inhibits BRAF ^V600E, CRAF, *MEK, and BRAF* (IC₅₀: 8.2, 56, 160 nM, and 190 nM, respectively).

HY-132844

Tunlametinib HL-085	MEK	Cancer
Tunlametinib is a highly selective, orally active *MEK1/2* inhibitor (IC₅₀=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRAS ^G12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .

HY-N6670

Cefotetan	Antibiotic Raf ERK Ras MEK Bacterial	Infection
Cefotetan is a binding agent that targets *human Raf1 kinase inhibitor protein* (hRKIP). Cefotetan binds to hRKIP, reduces the binding space between hRKIP and Raf1 kinase, relieves hRKIP's inhibition of the *Ras/Raf1/MEK/ERK* signaling pathway, and enhances ERK phosphorylation. Cefotetan can be used to study diseases associated with dysregulated Ras/Raf1/MEK/ERK signaling pathways. Cefotetan is also a broad-spectrum antibacterial agent that disrupts cell wall synthesis by binding to bacterial penicillin-binding proteins (PBPs). It is used to study bacterial infections such as bone, skin, urinary tract, and lower respiratory tract .

HY-158115

NST-628	Molecular Glues Raf MEK	Cancer
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .

HY-157750

MEK1/C-Raf-IN-1	MEK Raf	Cancer
MEK1/C-Raf-IN-1 (Compound 14d) is a *MEK1/C-Raf* inhibitor with IC₅₀ values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity .

HY-162873

MEK/RAF-IN-1	MEK Raf	Cancer
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both *MEK* and *RAF. It shows potent inhibition with IC₅₀* values of 28 nM for *MEK1, and 3 nM each for BRAF* and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .

HY-157740

XSJ-10	HDAC	Cancer
XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC_{50_s} of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 .

HY-18652A

Avutometinib potassium Ro 5126766 potassium; CH5126766 potassium	Raf MEK	Cancer
Avutometinib (CH5126766) (potassium) is a *RAF/MEK* clamp that potently inhibits *RAF/MEK* kinase activity and induces dominant negative *RAF-MEK* complexes preventing phosphorylation of *MEK* by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .

HY-177081

Envometinib	MEK	Cancer
Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma .

HY-W065835

2-Bromoaldisine	HIV	Infection
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits *Raf/MEK/MAPK* pathway .

HY-113632

Debromohymenialdisine 10Z-Debromohymenialdisine	Raf MEK	Cancer
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC₅₀ value of 881 nM in the initial *Raf/MEK-1/MAPK* signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation .

HY-10542

GW 5074 Maximum Cited Publications 7 Publications Verification	Raf Apoptosis	Cancer
GW 5074 is a potent and selective *c-Raf* inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms .

HY-141523

Vociprotafib RMC-4630; SHP2-IN-7	SHP2 Phosphatase	Cancer
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the *RAS-RAF-MEK-ERK* signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .

HY-142160

GNE-9815	Raf	Cancer
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K_i values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with *MEK* inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .

HY-174851

KRAS G12C-IN-70	Ras	Cancer
KRAS G12C-IN-70 is a selective KRAS G12C mutant inhibitor. KRAS G12C-IN-70 blocks KRAS G12C-mediated downstream signaling pathways (e.g., RAF-MEK-ERK) and inhibits tumor cell proliferation. KRAS G12C-IN-70 is promising for research of KRAS G12C mutation-related tumors (such as non-small cell lung cancer, colorectal cancer) .

HY-N0226

Epiberberine	Cholinesterase (ChE) Beta-secretase	Neurological Disease Metabolic Disease
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .

HY-N0226A

Epiberberine chloride 4 Publications Verification	Cholinesterase (ChE) Beta-secretase Reactive Oxygen Species (ROS)	Neurological Disease Metabolic Disease
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .

HY-12316

20(S)-Hydroxycholesterol 2 Publications Verification 20α-Hydroxycholesterol	Smo Endogenous Metabolite	Cardiovascular Disease Metabolic Disease Cancer
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the *Raf/MEK/ERK* pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .

HY-164529

SJ-C1044	Raf Ras MEK ERK VEGFR Tie c-Fms	Cancer
SJ-C1044 is an orally available *pan-RAF* inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and *MEK-ERK* phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .

HY-B0766

Bicyclol SY801	Autophagy Apoptosis HBV HCV HSP Reactive Oxygen Species (ROS) Bcl-2 Family Glutathione S-transferase p38 MAPK NF-κB Microtubule/Tubulin ERK JNK TNF Receptor Interleukin Related CDK Cyclin G-associated Kinase (GAK) mTOR P-glycoprotein Ferroptosis	Infection Inflammation/Immunology Cancer
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the *Ras/Raf/MEK/ERK* pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .

Cat. No.	Product Name

HY-L010

MAPK Compound Library	785 compounds
MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers. MCE designs a unique collection of 785 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

MAPK Compound Library

785 compounds

MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.

MCE designs a unique collection of 785 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

HY-L101

Anti-Liver Cancer Compound Library	2,383 compounds
Liver cancer is one of the leading malignancies which occupies the second position in cancer deaths worldwide, becoming serious threat to human health. Hepatocellular carcinoma (HCC), also known as hepatoma is the most common type accounting for approximately 90% of all liver cancers. Current evidence indicates that during hepatocarcinogenesis, two main pathogenic mechanisms prevail: (1) cirrhosis associated with hepatic regeneration after tissue damage caused by hepatitis infection, toxins or metabolic influences, and (2) mutations occurring in single or multiple oncogenes or tumor suppressor genes. Both mechanisms have been linked with alterations in several important cellular signaling pathways. These include the RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, WNT/b-catenin pathway, insulin-like growth factor pathway, c-MET/HGFR pathway , etc. MCE offers a unique collection of 2,383 compounds with identified and potential anti-liver cancer activity. MCE anti-liver cancer compound library is a useful tool for anti-liver cancer drugs screening and other related research.

Anti-Liver Cancer Compound Library

2,383 compounds

Liver cancer is one of the leading malignancies which occupies the second position in cancer deaths worldwide, becoming serious threat to human health. Hepatocellular carcinoma (HCC), also known as hepatoma is the most common type accounting for approximately 90% of all liver cancers.

Current evidence indicates that during hepatocarcinogenesis, two main pathogenic mechanisms prevail: (1) cirrhosis associated with hepatic regeneration after tissue damage caused by hepatitis infection, toxins or metabolic influences, and (2) mutations occurring in single or multiple oncogenes or tumor suppressor genes. Both mechanisms have been linked with alterations in several important cellular signaling pathways. These include the RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, WNT/b-catenin pathway, insulin-like growth factor pathway, c-MET/HGFR pathway , etc.

MCE offers a unique collection of 2,383 compounds with identified and potential anti-liver cancer activity. MCE anti-liver cancer compound library is a useful tool for anti-liver cancer drugs screening and other related research.

2-Bromoaldisine	Structural Classification Alkaloids Pyrrole Alkaloids Marine natural products Source classification	HIV
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits *Raf/MEK/MAPK* pathway .

Epiberberine chloride 4 Publications Verification	Alkaloids Structural Classification Neurological Disease Classification of Application Fields Coptis chinensis Franch. Ranunculaceae Source classification Metabolic Disease Plants Isoquinoline Alkaloids Disease Research Fields	Cholinesterase (ChE) Beta-secretase Reactive Oxygen Species (ROS)
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .

20(S)-Hydroxycholesterol 2 Publications Verification 20α-Hydroxycholesterol	Structural Classification Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids Cancer	Smo Endogenous Metabolite
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the *Raf/MEK/ERK* pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .

Debromohymenialdisine 10Z-Debromohymenialdisine	Structural Classification Natural Products Classification of Application Fields Marine natural products Sponge Disease Research Fields Cancer	Raf MEK
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC₅₀ value of 881 nM in the initial *Raf/MEK-1/MAPK* signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation .

Epiberberine	Alkaloids Source classification Ranunculaceae Coptis chinensis Franch. Plants Isoquinoline Alkaloids	Cholinesterase (ChE) Beta-secretase
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .

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