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Mlkl-/- NIH-3T3

" in MedChemExpress (MCE) Product Catalog:

100

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1

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1

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2

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11

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2

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Isotope-Labeled Compounds

6

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3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10331
    Regorafenib
    85+ Cited Publications

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET c-Kit FGFR Tie Cancer
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity .
    Regorafenib
  • HY-10261
    Afatinib
    100+ Cited Publications

    BIBW 2992

    EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK Cancer
    Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
    Afatinib
  • HY-100573
    Necrosulfonamide
    Maximum Cited Publications
    139 Publications Verification

    Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Interleukin Related NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways .
    Necrosulfonamide
  • HY-10261A
    Afatinib dimaleate
    100+ Cited Publications

    BIBW 2992MA2

    EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK Cancer
    Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
    Afatinib dimaleate
  • HY-112292
    GW806742X
    20+ Cited Publications

    Mixed Lineage Kinase VEGFR Others
    GW806742X, 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 has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis .
    GW806742X
  • HY-101524
    TC13172
    3 Publications Verification

    Mixed Lineage Kinase Cancer
    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells .
    TC13172
  • HY-N2909

    NF-κB RIP kinase Mixed Lineage Kinase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models .
    Aurantiamide
  • HY-10331A
    Regorafenib monohydrate
    85+ Cited Publications

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET FGFR c-Kit Tie Cancer
    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity .
    Regorafenib monohydrate
  • HY-144828
    RIP1/RIP3/MLKL activator 1
    5+ Cited Publications

    RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability .
    RIP1/RIP3/MLKL activator 1
  • HY-N0546
    Ligustroflavone
    2 Publications Verification

    Nuezhenoside

    CaSR RIP kinase Mixed Lineage Kinase TGF-beta/Smad Cardiovascular Disease Neurological Disease Metabolic Disease Endocrinology
    Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis .
    Ligustroflavone
  • HY-145574

    WX-0593

    Anaplastic lymphoma kinase (ALK) ROS Kinase BCRP Akt ERK STAT Cancer
    Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer .
    Iruplinalkib
  • HY-N0660

    Apoptosis PARP Caspase AMPK Autophagy VEGFR Keap1-Nrf2 STING 11β-HSD Ferroptosis PI3K Akt p38 MAPK ERK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
    Jujuboside B
  • HY-156591

    PROTACs Mixed Lineage Kinase Necroptosis Others
    PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death .
    PROTAC MLKL Degrader-1
  • HY-161247

    5-HT Receptor Metabolic Disease
    5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
    5-HT2A antagonist 2
  • HY-24504

    Mixed Lineage Kinase Inflammation/Immunology Cancer
    MBA-m1 is a MLKL inhibitor. MBA-m1 inhibits necroptosis in Mlkl −/− NIH-3T3 cells. MBA-m1 ameliorates disease in MLKL-induced dermatitis and abdominal aortic aneurysm mouse model .
    MBA-m1
  • HY-137191

    EGFR Cancer
    CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
    CH7233163
  • HY-108636

    MDM-2/p53 RIP kinase Mixed Lineage Kinase Reactive Oxygen Species (ROS) Necroptosis Cancer
    RETRA is a RIPK1/RIPK3/MLKL and p73 activator. RETRA mediates plasma membrane disruption, induces ROS accumulation, triggers early mitochondrial hyperpolarization, and synergistically drives necroptosis. RETRA inhibits cancer cells carrying mutant p53 via a p73-dependent salvage pathway. RETRA can be used in research related to cervical cancer and cancers with mutant p53 .
    RETRA
  • HY-151976
    STAT3-IN-15
    1 Publications Verification

    STAT Inflammation/Immunology
    STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibits STAT3 phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced by TGF-β1 and inhibit epithelial-mesenchymal transition (EMT) .
    STAT3-IN-15
  • HY-100573A
    (E/Z)-Necrosulfonamide
    1 Publications Verification

    Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Interleukin Related NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    (E/Z)-Necrosulfonamide
  • HY-177119

    PROTACs RIP kinase Mixed Lineage Kinase Infection Inflammation/Immunology
    ZBP1 Covalent PROTAC-1 is a covalent Z-DNA binding protein 1 ZBP1 PROTAC degrader, with its DC50 being 25.69 nM. ZBP1 Covalent PROTAC-1 integrates the ligand that recruits the VHL E3 ubiquitin ligase and the DNA aptamer (Aptamer Z3) with the specific Zα domain that can bind to ZBP1, which has a high affinity (KD = 2.71 nM) with ZBP1. After degrading ZBP1, the phosphorylation levels of downstream signaling molecules RIPK3 and MLKL significantly decrease. ZBP1 Covalent PROTAC-1, encapsulated by nano-liposomes, significantly improves the survival rate of mice infected with influenza A virus (IAV) after administration via the trachea .
    ZBP1 Covalent PROTAC-1
  • HY-156119

    Mixed Lineage Kinase Necroptosis Metabolic Disease Cancer
    MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects .
    MLKL-IN-6
  • HY-141889

    Mixed Lineage Kinase Inflammation/Immunology
    MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i) .
    MLKL-IN-2
  • HY-162424

    RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    ZBP1/RIP3/MLKL activator 1 (compound 3a) is a synthetically derived quinoline compound. ZBP1/RIP3/MLKL Activator 1 induces DNA damage, enhances intracellular levels of reactive oxygen species (ROS), and triggers apoptosis via the caspase pathway. Furthermore, when apoptosis is inhibited, ZBP1/RIP3/MLKL Activator 1 promotes necroptotic cell death through the ZBP1-RIP3-MLKL pathway. ZBP1/RIP3/MLKL Activator 1 is utilized in oncological research, particularly in the selective targeting of cells with impaired apoptotic function .
    ZBP1/RIP3/MLKL activator 1
  • HY-115489

    Ras Cancer
    GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM .
    GGTI-286
  • HY-115489A

    Protein Prenyltransferase Cancer
    GGTI-286 TFA, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 TFA selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 TFA also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM .
    GGTI-286 TFA
  • HY-112292A
    GW806742X hydrochloride
    20+ Cited Publications

    Mixed Lineage Kinase VEGFR Cancer
    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 hydrochloride retards MLKL membrane translocation and inhibits necroptosis .
    GW806742X hydrochloride
  • HY-124429

    ERK Cancer
    FQI1 is a Late SV40 Factor (LSF) inhibitor. FQI1 inhibits cell proliferation, with IC50s of 3, 0.79, 6.3 μM for NIH/3T3, HeLa, A549 cells. FQI1 can be used for cancer research .
    FQI1
  • HY-178821

    ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
    ROCK2-IN-12
  • HY-16124

    TLK-286; TER286

    DNA-PK Apoptosis Cancer
    Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies .
    Canfosfamide
  • HY-N3007A

    Others Inflammation/Immunology
    (E)-Naringenin chalcone is an orally active anti-allergic agent. (E)-Naringenin chalcone also has antioxidant, anti-inflammatory activities. (E)-Naringenin chalcone can improve adipocyte functions. (E)-Naringenin chalcone inhibits histamine release from rat peritoneal mast cell .
    (E)-Naringenin chalcone
  • HY-148767

    Mixed Lineage Kinase Others
    MLKL-IN-5 is a potent MLKL inhibitor that mediates necroptosis .
    MLKL-IN-5
  • HY-108960

    P2X Receptor Interleukin Related Neurological Disease
    PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain .
    PPADS
  • HY-149393

    Mixed Lineage Kinase RIP kinase Cancer
    RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion .
    RIPK3-IN-3
  • HY-148365

    Mixed Lineage Kinase RIP kinase CDK Cancer
    NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression .
    NecroIr1
  • HY-148366

    Mixed Lineage Kinase RIP kinase CDK Cancer
    NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
    NecroIr2
  • HY-100573S

    Isotope-Labeled Compounds Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Integrin NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    Necrosulfonamide-d4
  • HY-10261R

    BIBW 2992 (Standard)

    Reference Standards EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK Cancer
    Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
    Afatinib (Standard)
  • HY-12316R
    20(S)-Hydroxycholesterol (Standard)
    3 Publications Verification

    20α-Hydroxycholesterol (Standard)

    Reference Standards Smo Endogenous Metabolite Cancer
    20(S)-Hydroxycholesterol (Standard) is the analytical standard of 20(S)-Hydroxycholesterol. This product is intended for research and analytical applications. 20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
    20(S)-Hydroxycholesterol (Standard)
  • HY-16906

    Src Cancer
    T338C Src-IN-2 is a mutant c-Src kinase inhibitor, with an IC50 of 317 nM against T338C c-Src, 57 nM against T338C/V323A c-Src, and 19 nM against T338C/V323S c-Src. T338C Src-IN-2 inhibits the kinase activity of endogenous cysteine gatekeeper MOK. T338C Src-IN-2 reduces global phosphotyrosine levels in v-Src-ES1-transformed NIH-3T3 cells .
    T338C Src-IN-2
  • HY-152472

    Trk Receptor Neurological Disease
    ENT-C225 is an effective activator of TrkB neurotrophin receptor. ENT-C225 has high effect on activating TrkB receptor (TrkBR), and has good physicochemical properties and neuroprotective properties .
    ENT-C225
  • HY-129767

    Eukaryotic Initiation Factor (eIF) Cancer
    CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity .
    CMLD012612
  • HY-173185

    RIP kinase Necroptosis Inflammation/Immunology
    RIP1-IN-1 is an orally active RIP1 inhibitor with strong RIP1 binding affinity (Kd: 110 nM). RIP1-IN-1 exhibits strong anti-necroptosis activity. RIP1-IN-1 effectively inhibits the formation of necrosomes by blocking the phosphorylation of RIP1, RIP3 and MLKL signaling pathways. RIP1-IN-1 inhibits necroptosis and can be used in the study of acute liver injury .
    RIP1-IN-1
  • HY-128041

    Hydroxyfarnesyl phosphate

    Farnesyl Transferase Others
    α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.
    alpha-Hydroxy farnesyl phosphonic acid
  • HY-151542

    Mixed Lineage Kinase Necroptosis RIP kinase Neurological Disease
    MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM . MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MLKL-IN-4
  • HY-151541

    Mixed Lineage Kinase Necroptosis Neurological Disease
    MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM . MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MLKL-IN-3
  • HY-178163

    Ferroptosis Necroptosis RIP kinase Reactive Oxygen Species (ROS) Mixed Lineage Kinase Inflammation/Immunology
    Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease .
    Zharp1-163
  • HY-169072

    PROTACs Mixed Lineage Kinase Cancer
    PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074) [1] .
    PROTAC MLKL Degrader-2
  • HY-144437

    TGF-β Receptor Cancer
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
    ALK5-IN-9
  • HY-117807

    Ras Farnesyl Transferase VEGFR Cancer
    A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion .
    A-176120
  • HY-161921

    Fungal Infection
    Antifungal agent 108 (compound 14d), an original imidazo[1,2-b]pyridazine derivative, shows potent antifungal activity against Madurella mycetomatis (MM55 strain) with an IC50 of 0.9 μM. Antifungal agent 108 exhibits an IC50 of 14.3 μM on cell viability of NIH-3T3 murine fibroblast .
    Antifungal agent 108

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