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Pathways Recommended: MAPK/ERK Pathway
Results for "

MAPK Kinase Kinase Kinase

" in MedChemExpress (MCE) Product Catalog:

122

Inhibitors & Agonists

2

Screening Libraries

1

Fluorescent Dyes

1

Biochemical Assay Reagents

9

Peptides

2

Inhibitory Antibodies

19

Natural
Products

56

Recombinant Proteins

2

Isotope-Labeled Compounds

100

Antibodies

1

Oligonucleotides

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10201
    Sorafenib
    280+ Cited Publications

    Bay 43-9006

    		 Raf VEGFR FLT3 Autophagy Apoptosis STAT Akt MMP Cadherin p38 MAPK ERK MEK PI3K PARP Bcl-2 Family Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
    Sorafenib
  • HY-10320
    Doramapimod
    50+ Cited Publications

    BIRB 796

    		 p38 MAPK Raf Autophagy Inflammation/Immunology Cancer
    Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM .
    Doramapimod
  • HY-10201A
    Sorafenib tosylate
    280+ Cited Publications

    Bay 43-9006 tosylate

    		 Raf VEGFR FLT3 Autophagy Apoptosis STAT Akt MMP Cadherin p38 MAPK ERK MEK PI3K PARP Bcl-2 Family Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
    Sorafenib tosylate
  • HY-10456
    TAK-715
    10+ Cited Publications

    		 p38 MAPK Casein Kinase Wnt Inflammation/Immunology
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
    TAK-715
  • HY-16558
    Butein
    Maximum Cited Publications
    6 Publications Verification

    2’,3,4,4’-tetrahydroxy Chalcone

    		 EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
    Butein
  • HY-N0632
    Esculentoside A
    2 Publications Verification

    		 COX NF-κB Inflammation/Immunology
    Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta . Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) . Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
    Esculentoside A
  • HY-N0031
    Plantamajoside
    2 Publications Verification

    		 NF-κB PI3K Akt Apoptosis Autophagy p38 MAPK Src Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects .
    Plantamajoside
  • HY-N6246
    Asperulosidic Acid

    		NF-κB ERK Inflammation/Immunology Cancer
    Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities . ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways .
    Asperulosidic Acid
  • HY-116035
    Nimbolide
    2 Publications Verification

    		 Wnt NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
    Nimbolide
  • HY-12072
    Lck Inhibitor
    3 Publications Verification

    		 Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis .
    Lck Inhibitor
  • HY-148065
    FMF-06-098-1

    		PROTACs Wee1 CDK AAK1 ULK MELK Itk IRAK Ephrin Receptor FGFR MAP4K p38 MAPK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
    FMF-06-098-1
  • HY-111820
    CK1-IN-1

    		Casein Kinase p38 MAPK Cardiovascular Disease
    CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis .
    CK1-IN-1
  • HY-111940
    LUT014

    		Raf p38 MAPK ERK Inflammation/Immunology
    LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy .
    LUT014
  • HY-172581
    Clifutinib

    		FLT3 Apoptosis Ras p38 MAPK PI3K Akt JAK STAT Cancer
    Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia .
    Clifutinib
  • HY-N0818
    Chikusetsusaponin Iva
    2 Publications Verification

    Calenduloside F

    		 Keap1-Nrf2 Infection Metabolic Disease Endocrinology Cancer
    Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects .
    Chikusetsusaponin Iva
  • HY-112181
    KO-947
    4 Publications Verification

    		 ERK Cancer
    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
    KO-947
  • HY-137092
    IACS-13909
    3 Publications Verification

    		 SHP2 Phosphatase Cancer
    IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .
    IACS-13909
  • HY-P6442
    Chemerin15

    		Chemerin Receptor Syk ERK Src p38 MAPK P-selectin Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Chemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury .
    Chemerin15
  • HY-107620
    PD 198306

    		MEK Neurological Disease
    PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects .
    PD 198306
  • HY-N2902
    Artocarpin

    		Reactive Oxygen Species (ROS) Cancer
    Artocarpin is an orally active apoptosis inducer. Artocarpin targets NF-κB, Erk1/2, p38 MAPK, AktS473, p53, Akt 1 kinase and Akt 2 kinase. Artocarpin induces reactive oxygen species (ROS) production, mediates p53-dependent and p53-independent apoptotic signaling pathways, induces G1-phase cell cycle arrest, and triggers autophagic cell death. Artocarpin exerts cytotoxic and bactericidal effects on cancer cells, reduces bacterial load, and exhibits anti-inflammatory, analgesic and anti-angiogenic activities .
    Artocarpin
  • HY-112401
    p38 MAP Kinase Inhibitor IV

    		p38 MAPK Inflammation/Immunology
    p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
    p38 MAP Kinase Inhibitor IV
  • HY-110193
    SPP-86
    2 Publications Verification

    		 RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SPP-86
  • HY-148061
    DB1113

    		PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK) Cancer
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity .
    DB1113
  • HY-160469
    INY-05-040

    		Akt PROTACs Cancer
    INY-05-040 is an AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 exhibits anti-cancer activity. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines. INY-05-040 can suppress AKT signaling and induces the stress mitogen-activated protein kinase (MAPK) c-Jun N-terminal kinase (JNK). INY-05-040 is effective for breast cancer lines with a low-baseline activation of stress MAPK pathway. INY-05-040 can be studied for anti-cancer research .
    INY-05-040
  • HY-P10954
    Link N peptide

    		p38 MAPK Others
    Link N peptide is a proteoglycan aggregates activator in the extracellular matrix. Link N peptide can selectively activate the p38 mitogen-activated protein kinase (MAPK) pathway to promote the expression of type I and II collagens in human intervertebral disc cells. Link N peptide is promising for research of intervertebral disc degeneration-related diseases .
    Link N peptide
  • HY-W015445
    SD-169

    		p38 MAPK Metabolic Disease
    SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
    SD-169
  • HY-N1745A
    3-Deoxysappanchalcone
    2 Publications Verification

    		 Influenza Virus Infection Inflammation/Immunology Cancer
    3-Deoxysappanchalcone is a kinase inhibitor and antiviral agent. 3-Deoxysappanchalcone directly targets MET, EGFR, AKT, mTOR, p38 MAPK, JNK, thrombin, FXa, and influenza virus neuraminidase, thereby regulating related signaling pathways. 3-Deoxysappanchalcone induces cell cycle arrest, ROS production, and apoptosis. 3-Deoxysappanchalcone exhibits anti-inflammatory, anti-allergic, anticoagulant, and antithrombotic activities. 3-Deoxysappanchalcone is applicable to research related to gefitinib-resistant lung cancer, esophageal squamous cell carcinoma, thrombosis, and influenza virus infection .
    3-Deoxysappanchalcone
  • HY-159190
    HRX-0233

    		MAPKAPK2 (MK2) Cancer
    HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
    HRX-0233
  • HY-112389
    p38 MAP Kinase Inhibitor III
    2 Publications Verification

    		 p38 MAPK Inflammation/Immunology
    p38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively .
    p38 MAP Kinase Inhibitor III
  • HY-136990
    GLPG0259

    		p38 MAPK Cancer
    GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
    GLPG0259
  • HY-135906
    CK2/ERK8-IN-1
    2 Publications Verification

    		 Casein Kinase ERK Pim DYRK Apoptosis Cancer
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .
    CK2/ERK8-IN-1
  • HY-119715
    AG-012986

    		CDK Apoptosis Inflammation/Immunology Cancer
    AG-012986 is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .
    AG-012986
  • HY-P10438
    TAT-Braftide

    		Raf Cancer
    TAT-Braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by TAT-Braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
    TAT-Braftide
  • HY-120595
    JNJ-49095397

    RV568

    		 p38 MAPK Src Inflammation/Immunology
    JNJ-49095397 (RV568) is an inhaled narrow-spectrum kinase inhibitor (NSKI) against both the α and γ isoforms of p38 MAPK. JNJ-49095397 also inhibits SRC kinase family, specifically haematopoietic kinase (HCK) JNJ-49095397 shows potent anti-inflammatory effects and can be used for the research of chronic obstructive pulmonary disease (COPD) and asthma .
    JNJ-49095397
  • HY-Z3832
    N-Methylparoxetine

    		Apoptosis p38 MAPK Autophagy Cancer
    N-Methylparoxetine is a derivative of Paroxetine that induces Apoptosis NSCLC cells by activating mitogen-activated protein kinase ( MAPK). N-Methylparoxetine has antitumor activity .
    N-Methylparoxetine
  • HY-160765
    WNTinib

    APS-8-100-2

    		 Wnt Apoptosis Cancer
    WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .
    WNTinib
  • HY-112345
    PD-089828

    		FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
    PD-089828
  • HY-P10414A
    Klotho-derived peptide 1 hydrochloride

    KP1 (human) hydrochloride

    		 TGF-beta/Smad p38 MAPK Inflammation/Immunology
    Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
    Klotho-derived peptide 1 hydrochloride
  • HY-131335
    p38α inhibitor 2

    		p38 MAPK Inflammation/Immunology
    p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
    p38α inhibitor 2
  • HY-148063
    DB0614

    		PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK Metabolic Disease
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-P10436
    Braftide

    		Raf Cancer
    Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .
    Braftide
  • HY-P10414
    Klotho-derived peptide 1

    KP1 (human)

    		 TGF-beta/Smad p38 MAPK Inflammation/Immunology
    Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
    Klotho-derived peptide 1
  • HY-P10072A
    MK2-IN-5 acetate

    Hsp25 Kinase inhibitor acetate; Mk2 pseudosubstrate acetate

    		 JNK HSP MAPKAPK2 (MK2) p38 MAPK ERK Others
    MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
    MK2-IN-5 acetate
  • HY-108645
    AL 8697

    		p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .
    AL 8697
  • HY-10071A
    Y-27632 hydrochloride hydrate
    Maximum Cited Publications
    399 Publications Verification

    		 ROCK NF-κB Apoptosis Autophagy Akt mTOR NADPH Oxidase Reactive Oxygen Species (ROS) PAK Ras Neurological Disease Inflammation/Immunology Cancer
    Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade .
    Y-27632 hydrochloride hydrate
  • HY-145025
    ERK1/2 inhibitor 3

    		ERK Inflammation/Immunology Cancer
    ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .
    ERK1/2 inhibitor 3
  • HY-120505
    ITZ-1

    		ERK p38 MAPK Inflammation/Immunology
    ITZ-1 is an orally active and selective extracellular signal-regulated kinase (ERK)-mitogen-activated protein kinase (MAPK) pathway inhibitor with an IC50 of 0.51 μM for inhibiting interleukin-1β (IL-1β)-induced matrix metalloproteinase-13 (MMP-13) production. ITZ-1 reduces MMP-13 expression and suppresses nitric oxide (NO)-induced chondrocyte apoptosi. ITZ-1 is promising for research of osteoarticular diseases .
    ITZ-1
  • HY-N12726
    Halociline

    		p38 MAPK MMP Infection Inflammation/Immunology Cancer
    Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum. Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .
    Halociline
  • HY-E70844
    MAP2K2 Recombinant Human Active Protein Kinase

    		MEK Cancer
    MAP2K2 (MEK2) is a dual specificity protein kinase that belongs to the MAP kinase kinase family. This kinase is known to play a critical role in mitogen growth factor signal transduction. MAP2K2 phosphorylates and thus activates MAPK1/ERK2 and MAPK3/ERK1. MAP2K2 Recombinant Human Active Protein Kinase is a recombinant MAP2K2 protein that can be used to study MAP2K2-related functions .
    MAP2K2 Recombinant Human Active Protein Kinase
  • HY-142452
    Pan-RAF kinase inhibitor 1

    		Raf Cancer
    Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B) .
    Pan-RAF kinase inhibitor 1

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