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Activators+and+Inhibitors

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141

Inhibitors & Agonists

1

Screening Libraries

1

Fluorescent Dye

15

Peptides

2

Inhibitory Antibodies

33

Natural
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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0141
    Parthenolide
    Maximum Cited Publications
    39 Publications Verification

    (-)-Parthenolide

    		 NF-κB Autophagy Mitophagy Apoptosis IKK Cancer
    Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
    Parthenolide
  • HY-15253
    Tiplaxtinin
    10+ Cited Publications

    PAI-039; Tiplasinin

    		 PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM .
    Tiplaxtinin
  • HY-B1232
    Metyrapone
    10+ Cited Publications

    Su-4885

    		 Endogenous Metabolite Cytochrome P450 Autophagy Neurological Disease Metabolic Disease Endocrinology Cancer
    Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
    Metyrapone
  • HY-101761
    TM5441
    5+ Cited Publications

    		 PAI-1 Apoptosis Cardiovascular Disease Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
    TM5441
  • HY-N1462
    Atractyloside potassium salt
    4 Publications Verification

    		 Chloride Channel Autophagy mTOR AMPK Cardiovascular Disease Metabolic Disease Cancer
    Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
    Atractyloside potassium salt
  • HY-101255
    ODQ
    10+ Cited Publications

    		 Guanylate Cyclase Apoptosis Cancer
    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells .
    ODQ
  • HY-132304
    CC-90005

    		PKC Inflammation/Immunology
    CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression .
    CC-90005
  • HY-B0111
    Drospirenone
    1 Publications Verification

    Dihydrospirorenone

    		 Progesterone Receptor Androgen Receptor Endocrinology Cancer
    Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
    Drospirenone
  • HY-13634A
    Ezatiostat
    Maximum Cited Publications
    8 Publications Verification

    TER199free base; TLK199

    		 Glutathione S-transferase Apoptosis Cancer
    Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment .
    Ezatiostat
  • HY-111056
    UK122 TFA
    1 Publications Verification

    		 Ser/Thr Protease Cancer
    UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion .
    UK122 TFA
  • HY-N0106
    (Rac)-Salvianic acid A sodium

    (Rac)-Danshensu sodium; (Rac)-Tanshinol sodium

    		 Keap1-Nrf2 NF-κB Mitochondrial Metabolism Apoptosis Infection Cardiovascular Disease Inflammation/Immunology
    (Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases .
    (Rac)-Salvianic acid A sodium
  • HY-15840
    YLF-466D
    2 Publications Verification

    C24

    		 AMPK Cancer
    YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
    YLF-466D
  • HY-N1504
    Loureirin B
    4 Publications Verification

    		 PAI-1 Potassium Channel ERK JNK Metabolic Disease
    Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
    Loureirin B
  • HY-W019721
    Cyclosporin D

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
    Cyclosporin D
  • HY-W018723
    4-Aminobenzamidine dihydrochloride
    1 Publications Verification

    p-Aminobenzamidine dihydrochloride

    		 Ser/Thr Protease PAI-1 Cardiovascular Disease Cancer
    4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study .
    4-Aminobenzamidine dihydrochloride
  • HY-16677A
    Mofegiline hydrochloride

    MDL72974A

    		 Monoamine Oxidase Neurological Disease
    Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) .
    Mofegiline hydrochloride
  • HY-N2963
    Broussonin E
    2 Publications Verification

    		 ERK p38 MAPK JAK STAT TNF Receptor Interleukin Related COX Arginase Inflammation/Immunology
    Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis .
    Broussonin E
  • HY-101214
    UK-371804

    		PAI-1 Inflammation/Immunology
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
    UK-371804
  • HY-133558
    VII-31
    2 Publications Verification

    		 E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways .
    VII-31
  • HY-101918
    DS-1040 Tosylate

    		Thrombin Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases .
    DS-1040 Tosylate
  • HY-N6023
    Thermopsoside

    		Cytochrome P450 Pregnane X Receptor (PXR) Others
    Thermopsoside is a CYP450 isoenzyme inhibitor and PXR activator. Thermopsoside inhibits CYP3A4, CYP2C19, CYP2D6 and CYP2C9 with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM and 32.0 μM, respectively .
    Thermopsoside
  • HY-100415
    UKI-1

    WX-UK1; UKI-1C

    		 PAI-1 Ser/Thr Protease Cancer
    UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells .
    UKI-1
  • HY-N0218
    Benzoylmesaconine
    1 Publications Verification

    Mesaconine 14-benzoate

    		 NF-κB Interleukin Related Inflammation/Immunology
    Benzoylmesaconine is a monoester-type alkaloid and is the most abundant component of Wutou decoction, which is widely used in China for rheumatoid arthritis. Benzoylmesaconine exhibits potent anti-inflammatory properties by inhibiting NF-κB. Benzoylmesaconine can suppress NLRP3 inflammasome activation by inhibiting IL-1β secretion and GSDMD-N protein expression. Benzoylmesaconine reduces intracellular K + efflux and disrupts NLRP3 inflammasome assembly .
    Benzoylmesaconine
  • HY-101042
    AG-494

    Tyrphostin AG 494

    		 EGFR CDK Cancer
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis .
    AG-494
  • HY-122098
    Diaplasinin

    PAI-749

    		 PAI-1 Cardiovascular Disease
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy .
    Diaplasinin
  • HY-N0518
    Toddalolactone
    1 Publications Verification

    		 PAI-1 Cardiovascular Disease
    Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM .
    Toddalolactone
  • HY-122714
    SK-216

    		PAI-1 Cancer
    SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma .
    SK-216
  • HY-177106
    ADT-1004

    		Drug Intermediate Ras Cancer
    ADT-1004 is an orally active prodrug of ADT-007 (HY-157887). ADT-007 is a reversible, highly potent and selective pan-RAS inhibitor that binds to the nucleotide-free conformation of RAS proteins and blocks their GTP activation, thereby inhibiting the downstream MAPK and AKT signaling pathways. ADT-1004 can be used for the research of pancreatic ductal adenocarcinoma .
    ADT-1004
  • HY-114330A
    ZK824859 hydrochloride

    		PAI-1 Ser/Thr Protease Inflammation/Immunology
    ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
    ZK824859 hydrochloride
  • HY-128403
    BTK inhibitor 8

    		Btk Inflammation/Immunology
    BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits Btk activity. BTK inhibitor 8 suppresses B cell activation. BTK inhibitor 8 is applicable to research related to arthritis and asthma .
    BTK inhibitor 8
  • HY-N0141R
    Parthenolide (Standard)

    (-)-Parthenolide (Standard)

    		 Reference Standards NF-κB Autophagy Mitophagy Apoptosis Cancer
    Parthenolide (Standard) is the analytical standard of Parthenolide. This product is intended for research and analytical applications. Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
    Parthenolide (Standard)
  • HY-155363
    AMPK activator 13

    		AMPK Metabolic Disease
    AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity .
    AMPK activator 13
  • HY-108047
    MK-0873

    		Phosphodiesterase (PDE) Metabolic Disease Inflammation/Immunology
    MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor. MK-0873 increases intracellular levels of cyclic adenosine phosphate (cAMP) by inhibiting the activity of the PDE4 enzyme and subsequently activates protein kinase A (PKA). Activated PKA inhibits the activity of inflammatory cells and leads to direct relaxation of airway smooth muscle. MK-0873 can be used in studies of chronic obstructive pulmonary disease (COPD) .
    MK-0873
  • HY-158196
    PERK/eIF2α activator 1

    		PERK Apoptosis Cancer
    PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
    PERK/eIF2α activator 1
  • HY-168929
    SHP1 activator 1

    		SHP1 Fluorescent Dye Phosphatase STAT Apoptosis Cancer
    SHP1 activator 1 (Compound 3n) is an activator for src homology-2 domain-containing protein tyrosine phosphatase 1(SHP1) with an EC50 of 17.66 μM. SHP1 activator 1 inhibits the proliferation of ABC-DLBCL cells, induces apoptosis by inhibiting STAT3 signaling pathway. SHP1 activator 1 emitts blue and green fluorescence signalis in MDA-MB-231 cell, and can be used as a cell imaging agent .
    SHP1 activator 1
  • HY-126361A
    ZK824190 hydrochloride
    1 Publications Verification

    		 Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
    ZK824190 hydrochloride
  • HY-126361
    ZK824190

    		Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
    ZK824190
  • HY-122052
    UK‑396082

    		Thrombin Metabolic Disease
    UK‑396082 is a potent thrombin activated fibrinolytic inhibitor (TAFI) inhibitor. UK‑396082 increases plasmin activity and induces a parallel decrease in ECM levels. UK‑396082 can be used in research of chronic kidney disease (CKD) .
    UK‑396082
  • HY-116868
    Anecortave acetate

    Anecortave

    		 PAI-1 Cardiovascular Disease
    Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases .
    Anecortave acetate
  • HY-P10234A
    Poneratoxin acetate
    3 Publications Verification

    		 Sodium Channel Neurological Disease
    Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
    Poneratoxin acetate
  • HY-149391
    PROTAC BTK Degrader-6

    		PROTACs Btk Inflammation/Immunology
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .
    PROTAC BTK Degrader-6
  • HY-121896
    DSHN

    		SHP2 Cancer
    DSHN is a potent small heterodimer partner (SHP) activator. DSHN inhibits Ccl2 expression and secretion by inhibiting p65 activation of Ccl2 promoter activity. DSHN can be used in research of cancer .
    DSHN
  • HY-113492
    5(S)15(S)-DiHETE
    1 Publications Verification

    		 Interleukin Related Cardiovascular Disease Inflammation/Immunology
    5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC50 of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis .
    5(S)15(S)-DiHETE
  • HY-144287
    Glucokinase activator 3

    		Glucokinase Sodium Channel Metabolic Disease
    Glucokinase activator 3 is an orally active Glucokinase (GK) activator with an AC50 of 38 nM. Glucokinase activator 3 inhibits hERG channel and sodium channel in patch clamp assays. Glucokinase activator 3 exhibits high efficacy in reducing blood glucose in diet-induced obese (DIO) mice. Glucokinase activator 3 has the potential for the research of type 2 diabetes .
    Glucokinase activator 3
  • HY-106508
    Fendosal

    HP 129; P 71-0129

    		 PAI-1 Inflammation/Immunology
    Fendosal (HP 129) is an orally active, potent non-steroidal anti-inflammatory agent. Fendosal (HP 129) is also an inhibitor of Plasminogen activator inhibitor-1 (PAI-1) .
    Fendosal
  • HY-164364A
    DOTAGA.(SA.FAPi)2 TFA

    		FAP Cancer
    DOTAGA.(SA.FAPi)2 TFA is a potent dimeric fibroblast-activation protein inhibitor (FAPi). DOTAGA.(SA.FAPi)2 TFA has the potential for cancer diagnosis research .
    DOTAGA.(SA.FAPi)2 TFA
  • HY-114330
    ZK824859

    		PAI-1 Ser/Thr Protease Inflammation/Immunology
    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
    ZK824859
  • HY-P10234
    Poneratoxin

    		Sodium Channel Neurological Disease
    Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
    Poneratoxin
  • HY-130073
    Amorfrutin A

    		NF-κB Apoptosis Cancer
    Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .
    Amorfrutin A
  • HY-N10312
    Yadanzigan

    YDZG

    		 NOD-like Receptor (NLR) NF-κB Reactive Oxygen Species (ROS) Inflammation/Immunology
    Yadanzigan (YDZG) is an anti-inflammatory agent and a NLRP3 inhibitor. Yadanzigan specifically inhibits NLRP3 activation via inhibiting NF-κB pathway and Reactive Oxygen Species production. Yadanzigan also moderates LPS (HY-D1056)-induced acute lung injury (ALI) in mice .
    Yadanzigan

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