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Pathways Recommended: PI3K/Akt/mTOR
Targets Recommended: MAP4K Na+/K+ ATPase MAP3K PI3K AMPK PI4K NKCC Ribosomal S6 Kinase (RSK) MEK

Results for "Amp k Inhibitors" in MCE Product Catalog:

563

Inhibitors & Agonists

5

Screening Libraries

2

Dye Reagents

2

Biochemical Assay Reagents

54

Peptides

100

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-15073
    Becampanel

    Amp 397

    iGluR Neurological Disease
    Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
  • HY-106723
    AMP-PCP

    HSP Cancer
    AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90.
  • HY-106723A
    AMP-PCP disodium

    HSP Cancer
    AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90.
  • HY-12326
    c-di-AMP

    Cyclic diadenylate; Cyclic-di-Amp

    STING Bacterial Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-12326A
    c-di-AMP sodium

    Cyclic diadenylate sodium; Cyclic-di-Amp sodium

    STING Bacterial Endogenous Metabolite Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-124151
    Adenosine-2'-monophosphate

    2'-Amp; Adenosine 2'-phosphate; Amp 2'-phosphate

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-128933
    AMP-PNP tetralithium

    Adenylyl-imidodiphosphate tetralithium

    Potassium Channel Metabolic Disease
    AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits KATP channels.
  • HY-N7517
    Adenosine 5′-monophosphoramidate sodium

    Nucleoside Antimetabolite/Analog Others
    Adenosine 5′-monophosphoramidate sodium is an adenosine derivative and can be used as an intermediate for nucleotide synthesis. Adenosine 5′-monophosphoramidate has a significant effect on the accumulation of cyclic AMP.
  • HY-14533
    K 01-162

    K162

    Amyloid-β Neurological Disease
    K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM.
  • HY-12512
    cGAMP

    Cyclic GMP-Amp; 3',3'-cGAmp

    STING Inflammation/Immunology
    cGAMP (Cyclic GMP-AMP; 3',3'-cGAMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.
  • HY-B1511
    Cyclic AMP

    Cyclic adenosine monophosphate; Adenosine cyclic 3', 5'-monophosphate; cAmp

    Endogenous Metabolite Others
    Cyclic AMP (cAMP) is a mitogenic messenger and promotes the G1 to S phase transition in the cell cycle.
  • HY-16349
    Nimorazole

    K-1900

    Parasite Antibiotic Infection Cancer
    Nimorazole (K-1900) is a nitroimidazole anti-infective.
  • HY-N2240
    Eupalinolide K

    STAT Cancer
    Eupalinolide K, a sesquiterpene lactones compound from Eupatorium lindleyanum, is a STAT3 inhibitor. Eupalinolide K is a Michael reaction acceptor (MRA) .
  • HY-N6736
    K-252c

    PKC Bacterial Apoptosis Cancer Infection
    K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
  • HY-119293
    K777

    Cathepsin CCR Cytochrome P450 Cancer Infection
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
  • HY-136352
    Adenosine 5'-succinate

    Others Others
    Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
  • HY-100400A
    K-604 dihydrochloride

    Acyltransferase Cardiovascular Disease
    K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.
  • HY-15779
    K145

    SPHK Apoptosis Cancer
    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
  • HY-N6734
    K-252b

    PKC Infection
    K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .
  • HY-U00422
    K-756

    PARP Cancer
    K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
  • HY-108717
    Protease K

    Others Others
    Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures.
  • HY-12743A
    K-7174 dihydrochloride

    Others Inflammation/Immunology
    K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-12743
    K-7174

    Others Inflammation/Immunology
    K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-N4176
    Ginkgolide K

    Autophagy Neurological Disease
    Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity.
  • HY-N4234
    Angelol K

    Others Inflammation/Immunology
    Angelol K is a natural product from Chinese angelica.
  • HY-15071
    YM90K

    iGluR Neurological Disease
    YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions.
  • HY-15685
    Ripasudil

    K-115

    ROCK Neurological Disease
    Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
  • HY-N0904
    Ginsenoside C-K

    Ginsenoside compound K; Ginsenoside K

    COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
  • HY-Y0241
    2-Cyanopyrimidine

    Cathepsin Metabolic Disease
    2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos.
  • HY-N2243
    Hosenkoside K

    Others Inflammation/Immunology
    Hosenkoside K is a baccharane glycoside isolated from the seeds of impatiens balsamina.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-15779A
    K145 hydrochloride

    SPHK Apoptosis Cancer
    K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
  • HY-18674
    K-Ras-IN-1

    Ras Cancer
    K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference)
  • HY-109569
    Vitamin K2

    Endogenous Metabolite Metabolic Disease
    Vitamin K2 is an endogenous metabolite.
  • HY-P1106
    K41498

    CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study.
  • HY-B1508
    Vitamin K4

    acetomenaphthone

    Endogenous Metabolite Apoptosis Cancer Cardiovascular Disease
    Vitamin K4 is a chemically synthesized Vitamin K which plays an important role in the normal blood coagulation system.
  • HY-112499
    Menaquinone-7

    Vitamin K2-7; Vitamin K2(35); Vitamin MK-7

    Others Cardiovascular Disease
    Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS).
  • HY-103647
    K00546

    CDK Cancer
    K00546 is a potent CDK1 and CDK2 inhibitor and is a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively. K00546 is also a triazole-1-carbothioamide inhibitor.
  • HY-12278
    K02288

    TGF-β Receptor Others
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
  • HY-B2172
    Vitamin K

    Others Cardiovascular Disease
    Vitamin K is a group of fat soluble vitamins, important for the function of numerous proteins within the body, such as the coagulation factors, osteocalcin and matrix-Gla protein.
  • HY-N5078
    Terrestrosin K

    Others Cardiovascular Disease
    Terrestrosin K, a steroidal saponin from Tribulus terrestris L., has potential to treat cardiovascular and cerebrovascular diseases.
  • HY-15125
    (R)-(+)-Bay-K-8644

    Calcium Channel Cardiovascular Disease
    (R)-(+)-Bay-K-8644 is a calcium channel inhibitor. (R)-(+)-Bay-K-8644 inhibits Ba 2+ currents (IBa) (IC50=975 nM).
  • HY-100564
    2',3'-cGAMP

    2'-3'-cyclic GMP-Amp

    Endogenous Metabolite STING IFNAR Metabolic Disease
    2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm.
  • HY-112191
    PI3K-IN-10

    PI3K Cancer
    PI3K-IN-10 is a potent pan-PI3K inhibitor as a benzimidazole derivative, compound 332, extracted from patent WO2018057808A1.
  • HY-115555
    K-Ras-PDEδ-IN-1

    Phosphodiesterase (PDE) Cancer
    K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM.
  • HY-101090
    KYA1797K

    Wnt β-catenin Cancer
    KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-15124
    (S)-(-)-Bay-K-8644

    Calcium Channel Cardiovascular Disease
    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca 2+ channel. (S)-(-)-Bay-K-8644 activates Ba 2+ currents (IBa) (EC50=32 nM).
  • HY-19966
    K858 (Racemic)

    Kinesin Apoptosis Cancer
    K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
  • HY-17402
    Nisoldipine

    BAY-k 5552

    Calcium Channel Reactive Oxygen Species Cardiovascular Disease
    Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  • HY-17451
    Glibornuride

    Potassium Channel Metabolic Disease
    Glibornuride is a blocker of ATP-sensitive K + channels (KATP channel) with a pKi of 5.75. Antidiabetic agent.
  • HY-101115
    PI3K-IN-6

    PI3K Cancer
    PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
  • HY-110385
    cGAMP disodium

    Cyclic GMP-Amp disodium; 3',3'-cGAmp disodium

    Endogenous Metabolite Inflammation/Immunology
    cGAMP disodium (Cyclic GMP-AMP disodium) is the third cyclic dinucleotide (CDN) to be discovered in bacteria. cGAMP disodium is an effective adjuvant for sublingual vaccination capable of promoting broad immunity including serum anti-PA neutralizing and anti-PA SIgA responses in airway secretions.
  • HY-125012
    MAP4K4-IN-3

    MAP4K Metabolic Disease
    MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent.
  • HY-114268
    BRD-K98645985

    HIV Infection
    BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity.
  • HY-129523
    PROTAC K-Ras Degrader-1

    PROTAC Ras Cancer
    PROTAC K-Ras Degrader-1 (Compound 518) is potent K-Ras degrader based PROTAC, exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-B0332
    Menadione

    Vitamin K3

    Endogenous Metabolite Others
    Menadione, a synthetic naphthoquinone, can be converted to active vitamin K2 in vivo.
  • HY-100564A
    2',3'-cGAMP sodium

    2'-3'-cyclic GMP-Amp sodium

    Endogenous Metabolite STING IFNAR Metabolic Disease
    2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm.
  • HY-U00186
    K134

    OPC33509

    Phosphodiesterase (PDE) Cardiovascular Disease
    K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
  • HY-B2156
    Menaquinone-4

    Vitamin K2(MK-4); Menaquinone K4

    Endogenous Metabolite Cancer
    Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
  • HY-N6732
    K-252a

    SF2370; Antibiotic K 252a; Antibiotic SF 2370

    PKC PKA CaMK Trk Receptor Autophagy Infection
    K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-100600
    BGG463

    K03859

    CDK Others
    BGG463 (K03859) is an orally active type II CDK2 inhibitor.
  • HY-136310
    PIP4K-IN-a131

    Others Cancer
    PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
  • HY-15004
    AUZ 454

    K03861

    CDK Cancer
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
  • HY-I0515
    Sofosbuvir impurity K

    HCV Infection
    Sofosbuvir impurity K, an diastereoisomer of Sofosbuvir, is the impurity of Sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
  • HY-18605
    K-Ras G12C-IN-2

    Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  • HY-B0254
    Glipizide

    CP 28720; K 4024

    Potassium Channel Metabolic Disease
    Glipizide(K 4024; CP 2872) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
  • HY-18606
    K-Ras G12C-IN-3

    Ras Cancer
    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
  • HY-15685A
    Ripasudil free base

    K-115 (free base)

    ROCK Neurological Disease
    Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
  • HY-131260
    Ibuprofen Impurity K

    COX Inflammation/Immunology
    Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-129776
    K-Ras ligand-Linker Conjugate 2

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-129775
    K-Ras ligand-Linker Conjugate 1

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-126810A
    NP213 TFA

    Fungal Infection
    NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections.
  • HY-130822
    K-Ras ligand-Linker Conjugate 4

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130823
    K-Ras ligand-Linker Conjugate 5

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130991
    K-Ras ligand-Linker Conjugate 6

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130707
    K-Ras ligand-Linker Conjugate 3

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-133124
    PARP/PI3K-IN-1

    PARP PI3K Apoptosis Cancer
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
  • HY-126810
    NP213

    Fungal Infection
    NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections.
  • HY-N0684
    Vitamin K1

    Phylloquinone; Phytomenadione

    Endogenous Metabolite Cardiovascular Disease
    Vitamin K1 a fat-soluble, naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.
  • HY-18604
    K-Ras G12C-IN-1

    Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
  • HY-128582
    PI3K/HDAC-IN-1

    PI3K HDAC Cancer
    PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively.
  • HY-18707
    K-Ras(G12C) inhibitor 12

    Ras Apoptosis Cancer
    K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.
  • HY-12068
    PI3K-IN-1

    XL-147 derivative 1

    PI3K Cancer
    PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.
  • HY-133029
    PI3K-IN-9

    PI3K Cancer
    PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM.
  • HY-111413
    c(phg-isoDGR-(NMe)k)

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-133114
    Ezetimibe ketone

    EZM-K

    Keap1-Nrf2 Autophagy Cancer Cardiovascular Disease
    Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
  • HY-111508
    PI3K/mTOR Inhibitor-2

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  • HY-112602
    PI3K/mTOR Inhibitor-1

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
  • HY-111413A
    c(phg-isoDGR-(NMe)k) TFA

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2

    GHSR
    K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-128771
    K-Ras G12C-IN-4

    Ras Cancer
    K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C.
  • HY-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
  • HY-100865
    BPR1K871

    DBPR114

    FLT3 Cancer
    BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy.
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA

    GHSR
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-15293B
    JTV-519 hemifumarate

    K201 hemifumarate

    Calcium Channel Cardiovascular Disease
    JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  • HY-101517
    PI3K-IN-2

    PI3K Cancer
    PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).
  • HY-A0181
    Adenosine monophosphate

    Amp

    Endogenous Metabolite Others
    Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
  • HY-12306
    8-Bromo-cAMP sodium salt

    8-Br-CAmp sodium salt

    PKA Cancer
    8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
  • HY-12831
    Ampkinone

    AMPK Metabolic Disease
    Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator.
  • HY-15293A
    JTV-519 free base

    K201 free base

    Calcium Channel Cardiovascular Disease
    JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  • HY-N1074
    Warangalone

    Scandenolone

    Parasite PKA Infection Inflammation/Immunology
    Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
  • HY-P0136
    SAMS

    AMPK Metabolic Disease
    SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
  • HY-B0272
    Rifampicin

    RifAmpin; Rifamycin Amp

    Bacterial Influenza Virus Antibiotic Infection
    Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
  • HY-107988
    MK-3903

    AMPK Metabolic Disease
    MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-15068
    NBQX

    FG9202

    iGluR Neurological Disease
    NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
  • HY-15068A
    NBQX disodium

    FG9202 disodium

    iGluR Neurological Disease
    NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
  • HY-U00136
    Win-62005

    Phosphodiesterase (PDE) Cardiovascular Disease
    Win-62005 is a cyclic AMP phosphodiesterase III (PDE III) inhibitor with Kis of 25 and 26 nM for rat heart and canine aorta, respectively.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-15979
    H-89

    Protein kinase inhibitor H-89

    PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
  • HY-16307
    MB05032

    Phosphatase Metabolic Disease
    MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.
  • HY-A0181A
    Adenosine 5'-monophosphate monohydrate

    5'-Amp monohydrate

    Adenosine Receptor HSV Infection Neurological Disease
    Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist. Adenosine 5'-monophosphate monohydrate has significant antiviral activity against HSV-1 and HSV-2.
  • HY-100126
    Tubercidin

    7-Deazaadenosine

    Bacterial DNA/RNA Synthesis Influenza Virus Antibiotic Infection
    Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
  • HY-113284
    Succinyladenosine

    N6-Succinyl adenosine

    Endogenous Metabolite Metabolic Disease
    Succinyladenosine, the metabolic product of dephosphorylation of intracellular adenylosuccinic acid (S-AMP) by cytosolic 5-nucleotidase, is a biochemical marker of adenylosuccinase (ASL) deficiency.
  • HY-B0283
    Acipimox

    K-9321

    Others Cardiovascular Disease
    Acipimox is a niacin derivative used as a hypolipidemic agent.
  • HY-P1350
    H-Lys-Trp-Lys-OH

    Bacterial Infection
    H-Lys-Trp-Lys-OH is a small molecule peptide which displays antibacterial and antiviral activities extracted from patent CN 104072579 A, Compound AMP12.
  • HY-128583
    G150

    Others Inflammation/Immunology
    G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-114182
    PF-06928215

    Others Inflammation/Immunology
    PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ. PF-06928215 has a high binding affinity of 0.2 μM (Kd).
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-B1730
    Phensuximide

    Others Metabolic Disease Neurological Disease
    Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-100412
    Linaprazan

    AZD0865

    Proton Pump Cancer
    Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding.
  • HY-18085
    Quercetin

    PI3K Autophagy Mitophagy Reactive Oxygen Species Apoptosis Cancer
    Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
  • HY-N0146
    Quercetin dihydrate

    PI3K Apoptosis Inflammation/Immunology Cancer
    Quercetin dihydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
  • HY-112435
    UCT943

    PI4K Infection
    UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.
  • HY-101333
    CPPG

    (RS)-CPPG

    mGluR Neurological Disease
    CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
  • HY-111754
    DMX-5804

    MAP4K Cardiovascular Disease
    DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
  • HY-10042
    Odanacatib

    MK-0822

    Cathepsin Metabolic Disease
    Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
  • HY-N0859
    Schisanhenol

    Schizanhenol; Gomisin-K3

    Others Cancer
    Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
  • HY-B0764A
    Bucladesine calcium

    Dibutyryl cAmp calcium salt; DBcAmp calcium salt

    PKA Phosphodiesterase (PDE) Apoptosis Others
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
  • HY-18085S
    Quercetin D5

    PI3K Autophagy Mitophagy Apoptosis Cancer
    Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
  • HY-19312
    3-Methyladenine

    3-MA

    PI3K Autophagy Mitophagy Endogenous Metabolite Cancer
    3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-13418A
    Dorsomorphin

    Compound C; BML-275

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
  • HY-100576
    NH125

    CaMK Autophagy Bacterial Fungal Virus Protease Cancer
    NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with an IC50 of 60 nM for eEF-2K.
  • HY-12016
    KU-55933

    ATM/ATR Autophagy Cancer
    KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
  • HY-P2289
    pBD-1

    Bacterial Infection
    pBD-1 is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs.
  • HY-110079
    TNP

    Others Cancer
    TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes.
  • HY-11006
    KU-57788

    NU7441

    DNA-PK CRISPR/Cas9 Cancer
    KU-57788 is a potent and selective inhibitor of DNA-PK with an IC50 of 13 nM, with selectivity over a range of kinases including mTOR, PI 3-K, ATM and ATR.
  • HY-100223
    Calpeptin

    Cathepsin Proteasome Apoptosis Inflammation/Immunology
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
  • HY-P2289A
    pBD-1 TFA

    Bacterial Infection
    pBD-1 TFA is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 TFA has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs.
  • HY-16705
    BRD4770

    Histone Methyltransferase Cancer
    BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
  • HY-19568
    Peficitinib

    ASP015K; JNJ-54781532

    JAK Inflammation/Immunology Cancer
    Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAmp sodium salt; DBcAmp sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • HY-12912
    KDU691

    PI4K Parasite Infection
    KDU691 is a PI4K inhibitor.
  • HY-U00222
    S3337

    Proton Pump Inflammation/Immunology
    S3337 is an H +, K +-ATPase inhibitor.
  • HY-15206
    Glibenclamide

    Glyburide

    Potassium Channel Autophagy Metabolic Disease
    Glibenclamide is a selective inhibitor of ATP-sensitive K+ channel.
  • HY-U00017
    Coumetarol

    Dicumoxane; Ph 137

    Others Metabolic Disease
    Coumetarol (Dicumoxane) is a vitamin K antagonist.
  • HY-16689
    VU 0240551

    Potassium Channel Others
    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  • HY-101069
    Y-26763

    Potassium Channel Cardiovascular Disease
    Y-26763 is a K + channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K + (KATP) channel activator.
  • HY-12283
    Rostafuroxin

    PST 2238

    Na+/K+ ATPase Cardiovascular Disease
    Rostafuroxin(PST 2238) is a antihypertensive compound; Na,K-ATPase antognist;displaced [3H]ouabain from the dogkidney Na+,K+-ATPase with IC50 of 1.5 nM.
  • HY-101918
    DS-1040 Tosylate

    Others 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.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-N0579
    Fraxin

    Fraxoside

    Phosphodiesterase (PDE) Inflammation/Immunology
    Fraxin isolated from Acer tegmentosum, F. ornus or A. hippocastanum, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-13595
    Chrysophanol

    Chrysophanic acid

    EGFR Cancer
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
  • HY-B0567
    Dequalinium Chloride

    Potassium Channel Infection
    Dequalinium Chloride is a selective blocker of apamin-sensitive K+ channels.
  • HY-B1014
    Acenocoumarol

    Others Cardiovascular Disease
    Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist.
  • HY-12493A
    LY-2584702 tosylate salt

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • HY-12493B
    LY-2584702 hydrochloride

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • HY-P2316
    Epinecidin-1 TFA

    Bacterial Antibiotic Infection
    Epinecidin-1 TFA is a multi-functional antimicrobial peptide (AMP) from Orange-spotted grouper (Epinephelus coioides). Epinecidin-1 TFA has antibacterial, antifungal, antiviral, anti-tumor, and immunomodulatory effects. Epinecidin-1 TFA has the potential to be an alternative for current antibiotics.
  • HY-112769
    EX229

    AMPK Metabolic Disease
    EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
  • HY-14255
    Levcromakalim

    (-)-Cromakalim; BRL 38227

    Potassium Channel Cardiovascular Disease
    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K + channel (KATP) activator.
  • HY-B0325
    Phenindione

    Rectadione

    Others Cardiovascular Disease
    Phenindione is an anticoagulant which functions as a Vitamin K antagonist.
  • HY-U00042
    SKF96067

    Proton Pump Inflammation/Immunology
    SKF96067 is a reversible inhibitor of the gastric H +/K +-ATPase.
  • HY-12493
    LY-2584702 free base

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • HY-103261
    SCH28080

    Proton Pump Endocrinology
    SCH28080 is a reversible, K +-competitive inhibitor of the gastric (H +/K +)-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.
  • HY-133533
    O-2050

    Cannabinoid Receptor
    O-2050 is a high affinity cannabinoid CB1 receptor silent antagonist. O-2050 also acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC50=40.4 nM). O-2050 antagonizes effects of CP-55940 in vitro.
  • HY-P1954
    Piscidin-1 (22-42)

    Bacterial Cancer Infection
    Piscidin-1 (22-42) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
  • HY-P2048A
    MOTS-c(human) acetate

    AMPK GLUT Metabolic Disease
    MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
  • HY-108596
    BL-1249

    Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
  • HY-11002
    CP-466722

    ATM/ATR Cancer
    CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
  • HY-100414
    Soraprazan

    BYK61359

    Proton Pump Others
    Soraprazan is a reversible, and fast-acting inhibitor of gastric H +/K + ATPase.
  • HY-B1109
    N-Acetylprocainamide

    Acecainide; NAPA

    Potassium Channel Drug Metabolite Cardiovascular Disease
    N-Acetylprocainamide is a class III antiarrhythmic, which blocks K + channels.
  • HY-114181
    IRAK4-IN-4

    IRAK Inflammation/Immunology
    IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-114180
    RU.521

    RU320521

    Others Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-14428
    ICG-001

    β-catenin Apoptosis Cancer
    ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
  • HY-P1954A
    Piscidin-1 (22-42) (TFA)

    Bacterial Infection
    Piscidin-1 (22-42) (TFA) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) (TFA) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
  • HY-120348
    ML67-33

    Potassium Channel Neurological Disease Cardiovascular Disease
    ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-17044A
    Duvelisib R enantiomer

    IPI-145 R enantiomer; INK1197 R enantiomer

    PI3K Cancer
    Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
  • HY-N3463
    Isopimaric acid

    Potassium Channel
    Isopimaric acid is a potent opener of large conductance calcium activated K + (BK) channels.
  • HY-P1978
    CysHHC10

    Bacterial Infection
    CysHHC10 is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
  • HY-106005
    MMV390048

    Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
  • HY-50887
    L-873724

    Cathepsin Metabolic Disease
    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
  • HY-14854
    Tecarfarin

    ATI-5923

    Others Cardiovascular Disease
    Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
  • HY-N2433
    Paederosidic acid methyl ester

    Potassium Channel Neurological Disease
    Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
  • HY-U00428A
    GNE 220 Hydrochloride

    MAP4K Cancer
    GNE 220 (Hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
  • HY-15868
    HS-173

    PI3K Apoptosis Cancer
    HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.
  • HY-107319
    Almitrine mesylate

    Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate

    Potassium Channel Neurological Disease Cardiovascular Disease
    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca 2+-dependent K + channel.
  • HY-B0542
    Ouabain Octahydrate

    Acocantherine; G-Strophanthin

    Na+/K+ ATPase Autophagy Cardiovascular Disease Cancer
    Ouabain Octahydrate is an inhibitor of Na +/K +-ATPase, used for the treatment of congestive heart failure.
  • HY-75839
    Dronedarone Hydrochloride

    Potassium Channel Autophagy Cardiovascular Disease
    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na +, K + and Ca 2+ currents.
  • HY-P1978A
    CysHHC10 TFA

    Bacterial Infection
    CysHHC10 TFA is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 TFA against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
  • HY-14854A
    Tecarfarin sodium

    ATI-5923 sodium

    Others Metabolic Disease
    Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin sodium has the antithrombotic activity.
  • HY-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-B2179
    Cloperastine fendizoate

    Potassium Channel Inflammation/Immunology
    Cloperastine fendizoate inhibits the hERG K + currents in a concentration-dependent manner with an IC50 value of 27 nM.
  • HY-U00428
    GNE 220

    MAP4K Cancer
    GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
  • HY-15718
    Istaroxime

    PST2744

    Na+/K+ ATPase Cardiovascular Disease
    Istaroxime (PST2744) is a potent inhibitor of Na +,K +-ATPase with IC50 of 0.11 μM.
  • HY-13425
    Deguelin

    (-)-Deguelin; (-)-cis-Deguelin

    Akt Autophagy Cancer
    Deguelin, a naturally occurring rotenoid, is a potent PI3K/AKT inhibitor.
  • HY-A0145
    Phenprocoumon

    Others Others
    Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
  • HY-B1446
    Esomeprazole magnesium

    (S)-Omeprazole magnesium; (-)-Omeprazole magnesium

    Proton Pump Others
    Esomeprazole magnesium is an inhibitor of H +, K +-ATPase, effectively used in the research of upper intestinal disorder.
  • HY-15384
    Picoprazole

    Proton Pump Metabolic Disease
    Picoprazole is a specific inhibitor of H +/K +-ATPase with IC50 of 3.1±0.4 μM.
  • HY-101625
    Recilisib

    Ex-RAD; ON 01210

    Akt PI3K Cancer
    Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
  • HY-B1357
    Digitoxin

    Na+/K+ ATPase Cardiovascular Disease
    Digitoxin is an effective Na+/K+-ATPase inhibitor, the EC50 value of Digitoxin is 0.78 μM.
  • HY-P0197
    Neurokinin A

    α-Neurokinin; Neuromedin L; Substance K

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin A acts via neurokinin 2 (NK-2) receptor.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-122635A
    T-448

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
  • HY-100332
    CP 375

    Others Others
    CP 375 is a Fe 3+ chelating agent, with a log K1 value of 14.50.
  • HY-108003
    MM 07

    Others Cardiovascular Disease
    MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart.
  • HY-16937
    ISA-2011B

    Others Cancer
    ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
  • HY-N6574
    Marinobufogenin

    Na+/K+ ATPase Cardiovascular Disease Metabolic Disease Neurological Disease
    Marinobufogenin is a strong inhibitor of Na +/K + ATPase that has been identified in mammalian plasma.
  • HY-100343
    GNE-495

    MAP4K Cancer
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
  • HY-N3584
    Paris saponin VII

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Cancer
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
  • HY-17623
    Tegoprazan

    Proton Pump Metabolic Disease
    Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro.
  • HY-117825
    RU-TRAAK-2

    Potassium Channel Neurological Disease
    RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).
  • HY-110150
    UNC3230

    Others Cancer Inflammation/Immunology
    UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
  • HY-135809
    A2764 dihydrochloride

    Potassium Channel Neurological Disease
    A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
  • HY-101664
    Ilaprazole

    IY-81149

    Proton Pump Metabolic Disease Cancer
    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H +/K +-ATPase with an IC50 of 6.0 μM.
  • HY-B2133
    Cloperastine hydrochloride

    Potassium Channel Inflammation/Immunology
    Cloperastine hydrochloride inhibits the hERG K + currents in a concentration-dependent manner with an IC50 value of 27 nM.
  • HY-107364
    MTX-211

    EGFR PI3K Cancer
    MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
  • HY-12496
    NS-1619

    Potassium Channel Cardiovascular Disease
    NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.
  • HY-100470
    NSC781406

    PI3K mTOR Cancer
    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
  • HY-B0325S
    Phenindione D5

    Rectadione D5

    Others Cardiovascular Disease
    Phenindione D5 is deuterium labeled Phenindione, which is an anticoagulant which functions as a Vitamin K antagonist.
  • HY-P1762
    Influenza NP (147-155)

    Influenza Virus Infection
    Influenza NP (147-155) is a K d restricted epitope from influenza nucleoprotein.
  • HY-15773
    PF-4708671

    Ribosomal S6 Kinase (RSK) Autophagy Cancer
    PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.
  • HY-101963
    AD80

    Raf Src Ribosomal S6 Kinase (RSK) RET Cancer
    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
  • HY-13100
    PF 03716556

    Potassium Channel Metabolic Disease
    PF 03716556 is a potent, and selective H +, K +-ATPase antagonist, with a pIC50 value of 6.009.
  • HY-P0249A
    Phe-Met-Arg-Phe amide trifluoroacetate

    Potassium Channel Neurological Disease
    Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K + current, with ED50 of 23 nM in the peptidergic caudodorsal neurons.
  • HY-N1381
    Periplocin

    Apoptosis Cancer Inflammation/Immunology
    Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
  • HY-P1422
    Spadin

    Potassium Channel Neurological Disease
    Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.
  • HY-122635
    T-448 free base

    Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
  • HY-17021B
    Esomeprazole potassium salt

    (S)-Omeprazole potassium

    Proton Pump Endocrinology
    Esomeprazole potassium salt is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  • HY-N1446
    Oleic acid

    9-cis-Octadecenoic acid; 9Z-Octadecenoic acid

    Na+/K+ ATPase Endogenous Metabolite Apoptosis Cancer Metabolic Disease
    Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na +/K + ATPase activator.
  • HY-B1302
    Quinidine hydrochloride monohydrate

    Potassium Channel Parasite Infection Cardiovascular Disease
    Quinidine hydrochloride monohydrate is an anti-arrythmic agent which is also a potent blocker of K + channel with an IC50 of 19.9 μM.
  • HY-P1762A
    Influenza NP (147-155) (TFA)

    Influenza Virus Infection
    Influenza NP (147-155) TFA is a K d restricted epitope from influenza nucleoprotein.
  • HY-13305
    MK-2048

    HIV HIV Integrase Infection
    MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
  • HY-17023
    Esomeprazole sodium

    (S)-Omeprazole sodium

    Proton Pump Endocrinology
    Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  • HY-12408
    6H05

    Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-12346
    FH1

    NSC 12407; BRD-K4477

    Others Others
    FH1(BRDK4477) is a small molecule that can enhance the functions of cultured hepatocytes.
  • HY-10683
    PKI-402

    PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • HY-101117
    EED226

    Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-15643A
    LY 303511 hydrochloride

    TNF Receptor Potassium Channel Cancer
    LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
  • HY-N6745
    Citreoviridin

    Na+/K+ ATPase Apoptosis Infection Cardiovascular Disease
    Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells.
  • HY-15643
    LY 303511

    TNF Receptor Potassium Channel Cancer
    LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
  • HY-P1422A
    Spadin TFA

    Potassium Channel Neurological Disease
    Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.
  • HY-13719
    Oleandrin

    Na+/K+ ATPase Apoptosis Cancer
    Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
  • HY-17021A
    Esomeprazole magnesium salt

    Proton Pump Endocrinology
    Esomeprazole magnesium salt is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  • HY-19341
    Compound 401

    DNA-PK Cancer
    Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
  • HY-N0083
    Betulin

    Trochol

    Fatty Acid Synthase (FASN) Apoptosis Endogenous Metabolite Cancer
    Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
  • HY-16916
    NS1643

    Potassium Channel Autophagy Others
    NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K(+) channels with an EC50 of 10.5 μM.
  • HY-12408A
    6H05 (TFA)

    Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-P1244
    Secretin (33-59), rat

    Secretin (rat)

    Glucagon Receptor Neurological Disease
    Secretin (33-59), rat is a 27-aa peptide, acts on secretin receptor, enhances the secretion of bicarbonate, enzymes, and K + from the pancreas.
  • HY-17421A
    Tenatoprazole sodium

    Tenatoprazole sodium salt

    Proton Pump Cardiovascular Disease
    Tenatoprazole sodium (TU-199 sodium) is a proton pump inhibitor; inhibits hog gastric H +/K +-ATPase with an IC50 of 6.2 μM.
  • HY-12763
    GNE-317

    PI3K mTOR Cancer
    GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
  • HY-111510
    IPI-3063

    PI3K Inflammation/Immunology
    IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.
  • HY-N6002
    3'-Hydroxypterostilbene

    Apoptosis Autophagy Cancer
    3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
  • HY-135899
    SIRT7 inhibitor 97491

    Sirtuin Apoptosis Cancer
    SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
  • HY-125108
    PHPS1 sodium

    Phosphatase Cancer Cardiovascular Disease
    PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
  • HY-100501
    M2698

    MSC2363318A

    Ribosomal S6 Kinase (RSK) Akt Cancer
    M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
  • HY-15648
    GSK-J1

    Histone Demethylase Cancer
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
  • HY-15648D
    GSK-J1 lithium salt

    Histone Demethylase Cancer
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
  • HY-126327
    UNC4976

    Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-W027968
    Coumarin-3-carboxylic Acid

    2-Oxochromene-3-carboxylic acid

    Others Cancer
    Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line.
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Endocrinology
    Vonoprazan Fumarate (TAK-438) is an orally active potassium-competitive acid blocker which inhibits H +, K +-ATPase activity with an IC50 of 19 nM.
  • HY-106855
    Almokalant

    H 234​/09

    Potassium Channel Cardiovascular Disease
    Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.
  • HY-13519
    TRAM-34

    Potassium Channel Neurological Disease
    TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K + channel (IKCa1) (Kd=20 nM).
  • HY-B1604
    Chloroprocaine hydrochloride

    2-Chloroprocaine hydrochloride

    Na+/K+ ATPase Neurological Disease
    Chloroprocaine hydrochloride (2-Chloroprocaine hydrochloride) is a potent inhibitor of Na,K-ATPase activity with an IC50 of 13 mM. Chloroprocaine hydrochloride blocks peripheral nerve.
  • HY-11042
    GNE-477

    PI3K mTOR Cancer
    GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
  • HY-15673
    KP-23172

    PI3K Akt Cancer
    KP-23172 is a PI3-K/Akt pathway inhibitor extracted from patent US7196083.
  • HY-15434
    NG25

    MAP4K MAP3K Cancer Inflammation/Immunology
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
  • HY-N0143
    Phlorizin

    Floridzin; NSC 2833

    SGLT Na+/K+ ATPase Metabolic Disease
    Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na +/K +-ATPase inhibitor.
  • HY-100381
    Nigericin sodium salt

    Potassium Channel NOD-like Receptor (NLR) Bacterial Antibiotic Cancer Infection
    Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H +, K +, and Pb 2+ ionophore, a NLRP3 activator.
  • HY-U00200
    Dicirenone

    SC26304

    Mineralocorticoid Receptor Metabolic Disease
    Dicirenone (SC26304) inhibits the effects of Aldosterone on urinary K +:Na + ratios and the binding of [ 3H]Aldosterone to renal cytoplasmic and nuclear receptors.
  • HY-P0191
    Charybdotoxin

    Potassium Channel Inflammation/Immunology
    Charybdotoxin, a 37-amino acid peptide isolated from venom of the scorpion Leiurus quinquestriatus var. hebraeus, is a K + channel blocker.
  • HY-N2033
    Chebulinic acid

    DNA/RNA Synthesis TGF-beta/Smad Proton Pump Infection
    Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
  • HY-P0249
    Phe-Met-Arg-Phe, amide

    Potassium Channel Neurological Disease
    Phe-Met-Arg-Phe, amide dose dependently (ED50=23 nM) activates a K + current in the peptidergic caudodorsal neurons.
  • HY-10294
    Relacatib

    SB-462795

    Cathepsin Cancer Metabolic Disease
    Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
  • HY-129622
    NH2-PEG5-C6-Cl

    PROTAC Linker Cancer
    NH2-PEG5-C6-Cl (K-7) is a PROTAC linker, which refers to the PEG composition. NH2-PEG5-C6-Cl can be used in the synthesis of a series of PROTACs, and it induces degradation of intracellular molecules by autophagy.
  • HY-108044
    ONO-5334

    Cathepsin SARS-CoV Metabolic Disease
    ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
  • HY-12782T
    ORY-1001(trans)

    Histone Demethylase Cancer
    ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • HY-N0663
    Talatisamine

    Potassium Channel Neurological Disease
    Talatisamine, a aconitum alkaloid,is specific K + channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.
  • HY-10114
    TGX-221

    PI3K Cancer
    TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
  • HY-108593
    BMS-191011

    BMS-A

    Potassium Channel Neurological Disease
    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca 2+-activated potassium (maxi-K) channel, effective in stroke models.
  • HY-100007
    Vonoprazan

    TAK-438 free base

    Proton Pump Endocrinology
    Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H +, K +-ATPase activity with an IC50 of 19 nM.
  • HY-15719
    NU 7026

    LY293646

    DNA-PK Apoptosis Cancer
    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
  • HY-B0135A
    Furosemide sodium

    NKCC Cancer Metabolic Disease
    Furosemide sodium is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.
  • HY-B0135
    Furosemide

    NKCC Metabolic Disease Cancer
    Furosemide is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.
  • HY-A0176
    Glisoxepide

    Potassium Channel Metabolic Disease Cardiovascular Disease
    Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.
  • HY-P0191A
    Charybdotoxin TFA

    Potassium Channel Inflammation/Immunology
    Charybdotoxin TFA, a 37-amino acid peptide isolated from venom of the scorpion Leiurus quinquestriatus var. hebraeus, is a K + channel blocker.
  • HY-N6064
    Polygalacin D

    Apoptosis IAP Cancer
    Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
  • HY-15718A
    Istaroxime hydrochloride

    PST2744 hydrochloride

    Na+/K+ ATPase Calcium Channel Cardiovascular Disease
    Istaroxime hydrochloride is a Na +/K +-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.
  • HY-19562
    PF-06260933

    MAP4K Inflammation/Immunology
    PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
  • HY-16355
    NVP-QAV-572

    PI3K Cancer
    NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.
  • HY-16516
    Vitamin CK3

    Others Cancer
    Vitamin CK3 is the combination of Vitamin C and vitamin K3 (100:1 ratio) and has been shown to inhibit tumor growth and lung metastasis.
  • HY-15872
    FTI-277

    Farnesyl Transferase Cancer
    FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
  • HY-15648A
    GSK-J2

    Histone Demethylase Cancer
    GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
  • HY-12895
    SKI V

    SPHK PI3K Apoptosis Cancer
    SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.
  • HY-13514
    TG 100713

    PI3K Cancer
    TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.
  • HY-P1244A
    Secretin (33-59), rat TFA

    Secretin (rat) (TFA)

    Glucagon Receptor Neurological Disease
    Secretin (33-59), rat (TFA) is a 27-aa peptide, which acts on secretin receptor, and enhances the secretion of bicarbonate, enzymes, and K + from the pancreas.
  • HY-U00416
    ARS-1323

    Ras Cancer
    ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
  • HY-12005
    Fingolimod hydrochloride

    FTY720

    LPL Receptor PAK Inflammation/Immunology Cancer
    Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride also is a pak1 activator.
  • HY-12343
    ML277

    CID-53347902

    Potassium Channel Cardiovascular Disease
    ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
  • HY-N0776
    Isorhamnetin

    3'-Methylquercetin

    MEK PI3K Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.
  • HY-17022
    Esomeprazole Magnesium trihydrate

    (S)-Omeprazole magnesium trihydrate

    Proton Pump Autophagy Others
    Esomeprazole Magnesium trihydrate ((S)-Omeprazole magnesium trihydrate) is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  • HY-B1897A
    Menadione bisulfite sodium

    Menadione sodium bisulfite; Vitamin K3 sodium bisulfite

    Others
    Menadione bisulfite (sodium) is used as an agent to induce acute oxidative stress, and to function as a plant-defense activator against several pathogens.
  • HY-10081
    GS-6201

    CVT-6883

    Adenosine Receptor Inflammation/Immunology
    GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
  • HY-11063
    Fingolimod

    FTY720 free base

    LPL Receptor PAK Cancer Inflammation/Immunology
    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  • HY-N6738
    Bafilomycin B1

    Bacterial Fungal Antibiotic Infection
    Bafilomycin B1 is a macrolide antibiotic isolated from Streptomyces sp, inhibits Gram-positive bacteria and fungi, and acts as an inhibitor of K +-dependent ATPase of E. coli.
  • HY-107365
    PQR-530

    PI3K mTOR Cancer
    PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
  • HY-15466
    CH5132799

    PI3K Cancer
    CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
  • HY-135667
    DHODH-IN-9

    Influenza Virus Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC50 of 7.4.
  • HY-18650
    KU 59403

    ATM/ATR Cancer
    KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
  • HY-100398
    PF-04979064

    PI3K mTOR Cancer
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
  • HY-B0790
    TAI-1

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-P1282
    Agitoxin-2

    Potassium Channel Neurological Disease
    Agitoxin-2 is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).
  • HY-U00417
    ARS-1630

    Ras Cancer
    ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
  • HY-15100
    Balicatib

    AAE581

    Cathepsin Inflammation/Immunology
    Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
  • HY-13866
    Ro 31-8220 mesylate

    Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate

    PKC Neurological Disease Cardiovascular Disease Cancer
    Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-13866A
    Ro 31-8220

    Bisindolylmaleimide IX

    PKC Neurological Disease Cardiovascular Disease
    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
  • HY-127019
    Nigericin

    Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Cancer Infection
    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
  • HY-14470
    Sibutramine hydrochloride monohydrate

    BTS 54-524 hydrochloride monohydrate

    Serotonin Transporter Potassium Channel Metabolic Disease Neurological Disease
    Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K + channel (KV)4.3 is 17.3 μM.
  • HY-N6017
    Bakkenolide A

    Others Cancer
    Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
  • HY-12030
    PIK-90

    PI3K DNA-PK Cancer
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
  • HY-130819
    Tos-PEG4-THP

    PROTAC Linker Cancer
    Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523).
  • HY-P1282A
    Agitoxin-2 TFA

    Potassium Channel Neurological Disease
    Agitoxin-2 TFA is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).
  • HY-13764
    Tetrandrine

    NSC-77037; d-Tetrandrine

    Calcium Channel Potassium Channel Cancer Inflammation/Immunology
    Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca 2+ current (ICa) and Ca 2+-activated K + current.
  • HY-N2618
    3-​O-​Acetyloleanolic acid

    Apoptosis Cancer
    3-O-Acetyloleanolic acid (3AOA), an oleanolic acid derivative isolated from the seeds of Vigna sinensis K., induces in cancer and also exhibits anti-angiogenesis activity.
  • HY-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride

    GABA Receptor Neurological Disease
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-101428
    NS-638

    Calcium Channel Neurological Disease
    NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
  • HY-12358
    Tpl2 Kinase Inhibitor 1

    MAP3K Cancer Inflammation/Immunology
    Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers.
  • HY-P1602
    Apidaecin IB

    Bacterial Infection
    Apidaecin IB is a insect antimicrobial peptide, with minimum inhibitory concentration (MIC) values of 8 μM for E. coli (ML35, O18K1H7 and ATCC 25922).
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide

    GABA Receptor Neurological Disease
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-15900
    Voxtalisib

    XL765; SAR245409

    PI3K mTOR Cancer
    Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-112075
    Lidoflazine

    Potassium Channel Calcium Channel Cardiovascular Disease
    Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K + channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia.
  • HY-U00201
    KRN4884

    Potassium Channel Cardiovascular Disease
    KRN4884 is a K + channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels.
  • HY-18690
    Enasidenib

    AG-221

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
  • HY-102048
    STAT5-IN-2

    STAT Cancer
    STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect.
  • HY-135407S
    N-Desethyl Oxybutynin D5 hydrochloride

    Drug Metabolite Neurological Disease
    N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K + channels.
  • HY-12046
    PIK-93

    PI4K PI3K Virus Protease Cancer
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
  • HY-15174
    Dactolisib Tosylate

    BEZ235 Tosylate; NVP-BEZ 235 Tosylate

    PI3K mTOR Autophagy Cancer
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
  • HY-100626
    WNK463

    Ser/Thr Protease Cancer
    WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.
  • HY-15416
    NS309

    Potassium Channel Cardiovascular Disease
    NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.
  • HY-18172A
    (+)-KCC2 blocker 1

    Potassium Channel Neurological Disease
    (+)-KCC2 blocker 1 is a selective K +-Cl - cotransporter KCC2 blocker with an IC50 of 0.4 μM. (+)-KCC2 blocker 1 is a benzyl prolinate and a enantiomer of KCC2 blocker 1.
  • HY-B1500
    2,2,2-Trichloroethanol

    Potassium Channel Neurological Disease
    2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-130241
    Reverse transcriptase-IN-1

    HIV Infection
    Reverse transcriptase-IN-1 (Compound 12z) is a diarylbenzopyrimidine (DABP) analogue and a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50 value of 13.7 nM against HIV-1 reverse transcriptase enzyme.
  • HY-136522
    S2116

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
  • HY-103369
    PG01

    CFTR Endocrinology
    PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin.
  • HY-108582
    Y-27152

    Potassium Channel Cardiovascular Disease
    Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
  • HY-16662
    Oncrasin-1

    Ras Apoptosis Cancer
    Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
  • HY-15872A
    FTI-277 hydrochloride

    Farnesyl Transferase Apoptosis Influenza Virus Cancer Infection
    FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibits hepatitis delta virus (HDV) infection.
  • HY-15136
    Lonafarnib

    Sch66336

    Farnesyl Transferase Autophagy Influenza Virus Cancer Infection
    Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib has anti-hepatitis delta virus (HDV) activities.
  • HY-18172
    KCC2 blocker 1

    Potassium Channel Neurological Disease
    KCC2 blocker 1 is an orally active and selective K +-Cl - cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate and has antiepileptic effect.
  • HY-12757
    YHO-13177

    BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-P0256
    Apamin

    Apamine

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-N7126
    Citronellal

    Others Neurological Disease
    Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway.
  • HY-N6688
    Verruculogen

    Potassium Channel Bacterial Antibiotic Infection
    Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
  • HY-13685
    Miltefosine

    HePC; Hexadecyl phosphocholine

    Akt HIV Infection Cancer
    Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
  • HY-101436A
    Sematilide hydrochloride

    CK-1752 hydrochloride

    Potassium Channel Cardiovascular Disease
    Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
  • HY-136615
    5-Hydroxydecanoate sodium

    Potassium Channel Neurological Disease
    5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.
  • HY-101436
    Sematilide

    CK-1752

    Potassium Channel Cardiovascular Disease
    Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
  • HY-N2070
    Acevaltrate

    Na+/K+ ATPase Neurological Disease
    Acevaltrate, isolated from Valeriana glechomifolia, inhibits the Na +/K +-ATPase activity in the rat kidney and brain hemispheres with IC50s of 22.8±1.1 μM and 42.3±1.0 μM, respectively.
  • HY-14848
    Naluzotan

    PRX 00023

    5-HT Receptor Potassium Channel Neurological Disease
    Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K + channel blocker, with IC50 of 3800 nM.
  • HY-U00193
    Ro18-5362

    Others Metabolic Disease
    Ro18-5362 is the less active prodrug of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H ++K +)-ATPase activity and associated proton translocation.
  • HY-101146
    SF2523

    PI3K Epigenetic Reader Domain DNA-PK Cancer
    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
  • HY-N2357
    Eudesmin

    (-)-Eudesmin; Eudesmine; (-)-Eudesmine

    Ribosomal S6 Kinase (RSK) Cancer Infection Metabolic Disease Inflammation/Immunology
    Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.
  • HY-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-136122
    Tubulin inhibitor 7

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
  • HY-13333
    NVP-BAG956

    BAG 956

    PI3K Cancer
    NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-109079A
    Abeprazan hydrochloride

    DWP14012 hydrochloride

    Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-15177
    PF-04691502

    PI3K mTOR Autophagy Cancer
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
  • HY-109198
    Zandelisib

    PI3K Cancer
    Zandelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.
  • HY-N0039
    Ginsenoside Rb1

    Gypenoside III

    Na+/K+ ATPase IRAK NF-κB Autophagy Mitophagy HSV Inflammation/Immunology Cancer
    Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na +, K +-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
  • HY-110153
    NS19504

    Potassium Channel Neurological Disease
    NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
  • HY-10290
    MK-0674

    Cathepsin Metabolic Disease
    MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
  • HY-108606
    PI-828

    PI3K Casein Kinase Cancer
    PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
  • HY-109079
    Abeprazan

    DWP14012

    Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • HY-70063
    Buparlisib

    BKM120; NVP-BKM120

    PI3K Apoptosis Cancer
    Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
  • HY-13808
    UNC 0631

    Histone Methyltransferase Cancer
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
  • HY-130821
    THP-PEG4-Pyrrolidine(N-Me)-CH2OH

    PROTAC Linker Cancer
    THP-PEG4-Pyrrolidine(N-Me)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523).
  • HY-130820
    THP-PEG4-Pyrrolidine(N-Boc)-CH2OH

    PROTAC Linker Cancer
    THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523).
  • HY-P0256A
    Apamin TFA

    Apamine TFA

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-80012
    SJB3-019A

    Deubiquitinase Cancer
    SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-N6674
    Diazepinomicin

    ECO-4601; TLN-4601; BU 4664L

    Ras Apoptosis Cancer
    Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
  • HY-13026
    Idelalisib

    CAL-101; GS-1101

    PI3K Autophagy Cancer
    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
  • HY-17468S
    Bumetanide D5

    NKCC Cardiovascular Disease
    Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na +-K +-Cl - (NKCC1) inhibitor, weakly inhibits NKCC2, with  IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
  • HY-13260
    CCT128930

    Akt Autophagy Cancer
    CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
  • HY-102052
    DCEBIO

    Potassium Channel Inflammation/Immunology
    DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl secretion in T84 colonic cells. DCEBIO stimulates Cl secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl conductance.
  • HY-50847
    ZSTK474

    PI3K Autophagy Cancer
    ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
  • HY-19962
    Paxalisib

    GDC-0084

    PI3K mTOR Cancer
    Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
  • HY-N3354
    Lupiwighteone

    Apoptosis Cancer
    Lupiwighteone is an isoflavone present widely in wild-growing plants, with antioxidant, antimicrobial and anticancer effects. Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway.
  • HY-13504
    PIK-293

    PI3K Cancer Metabolic Disease
    PIK-293, an analog of IC87114, is a PI3K inhibitor, with IC50 values of 0.24 μM, 10 μM, 25 μM and 100 μM for p110δ, p110β, p110γ and p110α, respectively.
  • HY-12235
    PI-3065

    PI3K Inflammation/Immunology Cancer
    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
  • HY-B0422
    Nateglinide

    A4166; Senaglinide

    Potassium Channel Dipeptidyl Peptidase Metabolic Disease
    Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1] [2] .
  • HY-131055
    Mytoxin B

    ADC Cytotoxin PI3K Apoptosis Cancer
    Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
  • HY-N2491
    Deoxyelephantopin

    NF-κB Cancer
    Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
  • HY-101379A
    8-Bromo-cGMP sodium

    Calcium Channel Neurological Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator and significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects.
  • HY-14362
    GSK-25

    ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
  • HY-N2051
    Zeylenone

    Apoptosis Cancer
    Zeylenone, isolated from ethanol extract of the leaves of Uvaria grandiflora Roxb. Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways.
  • HY-N0877
    Bufalin

    Na+/K+ ATPase Cancer
    Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
  • HY-P0190
    Iberiotoxin

    Potassium Channel Cardiovascular Disease
    Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
  • HY-17468
    Bumetanide

    Ro 10-6338; PF 1593

    NKCC Cardiovascular Disease
    Bumetanide (Ro 10-6338;PF 1593) is a selective Na +-K +-Cl - cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
  • HY-N0479
    Licarin B

    (-)-Licarin B

    PPAR GLUT Metabolic Disease
    Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-P1320A
    [Nphe1]Nociceptin(1-13)NH2 TFA

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-W003467
    Rabeprazole Sulfide

    Proton Pump Bacterial Infection Inflammation/Immunology
    Rabeprazole Sulfide is an active metabolite of Rabeprazole. Rabeprazole is a proton pump inhibitor that suppresses gastric acid secretion through an interaction with (H +/K +)-ATPase in gastric parietal cells. Rabeprazole markedly inhibits the motility of H. pylori. Rabeprazole has the potential for various peptic diseases treatment.
  • HY-N7031
    (±)​-​Vasicine

    (±)​-Peganine

    Proton Pump Inflammation/Immunology
    (±)-Vasicine is the racemate of Vasicine. Vasicine (Peganine), isolated from Peganum harmala seeds, significantly inhibits H +-K +-ATPase activity in vitro with an IC50 of 73.47 μg/mL. Anti-ulcer activity. Vasicine shows significant anti-secretory, antioxidant and cytoprotective effect.
  • HY-136546
    Stafia-1

    STAT Cancer
    Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
  • HY-N5112B
    β,β-Dimethylacrylshikonin

    Others Cancer
    β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity.
  • HY-P0175A
    740 Y-P TFA

    740YPDGFR TFA; PDGFR 740Y-P TFA

    PI3K Autophagy Cancer
    740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  • HY-111383
    LX2343

    Beta-secretase PI3K Amyloid-β Autophagy Neurological Disease
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of clearance.
  • HY-128781
    Glucagon receptor antagonists-5

    Glucagon Receptor Metabolic Disease
    Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-101938
    Sinefungin

    Adenosyl-Ornithine; A-9145; Antibiotic 32232RP

    Histone Methyltransferase Fungal Antibiotic Infection Inflammation/Immunology
    Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation.
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
  • HY-101667
    LTURM34

    DNA-PK Cancer
    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  • HY-N6775
    Sonolisib

    PX-866

    PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-125292
    NV03

    Histone Methyltransferase Ligand for E3 Ligase Cancer
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
  • HY-103583
    KDU731

    PI4K Parasite Infection
    KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo. KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety.
  • HY-15280
    GSK2292767

    PI3K Inflammation/Immunology
    GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-114645
    PDK1-IN-RS2

    PDK-1 Cancer
    PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.
  • HY-103023
    CLP290

    Potassium Channel Neurological Disease
    CLP290 is an orally available activator of the neuron-specific K +-Cl cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
  • HY-B0563C
    Ropivacaine mesylate

    Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine mesylate is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine mesylate is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine mesylate inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension.
  • HY-16767
    Doravirine

    MK-1439

    HIV Reverse Transcriptase Infection
    Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
  • HY-123952
    RTC-5

    EGFR Cancer
    RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  • HY-W020468
    Linopirdine

    DuP 996

    Potassium Channel TRP Channel Neurological Disease
    Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
  • HY-B0563B
    Ropivacaine hydrochloride

    Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine hydrochloride is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine hydrochloride inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension.
  • HY-N2112
    Glaucocalyxin A

    PI3K Akt Apoptosis Cancer
    Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
  • HY-100869
    MM-589

    Histone Methyltransferase Cancer
    MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
  • HY-12330
    AZD8186

    PI3K Cancer
    AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
  • HY-N0728
    α-Linolenic acid

    PI3K Akt Cancer Cardiovascular Disease
    α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
  • HY-124798
    Rheb inhibitor NR1

    mTOR Cancer Inflammation/Immunology Neurological Disease
    Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 also is a selective mTORC1 inhibitor. NR1 inhibits the phosphorylation of T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner.
  • HY-114311
    FGFR1/DDR2 inhibitor 1

    FGFR Cancer
    FGFR1/DDR2 inhibitor 1 (compound 11k) is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
  • HY-10410
    TG101209

    FLT3 JAK RET Autophagy Apoptosis Cancer
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
  • HY-N0656A
    (+)-Usnic acid

    mTOR Cancer
    (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity.
  • HY-P1565
    Transdermal Peptide

    TD 1 (peptide)

    Na+/K+ ATPase Inflammation/Immunology
    Transdermal Peptide (TD 1 peptide) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide can enhance the transdermal delivery of many macromolecules.
  • HY-119322
    Tifenazoxide

    NN414

    Potassium Channel Metabolic Disease
    Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
  • HY-16952A
    Bepridil hydrochloride hydrate

    (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate

    Calcium Channel Cardiovascular Disease
    Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
  • HY-13431
    KU-0060648

    DNA-PK PI3K mTOR Cancer
    KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.
  • HY-A0154
    Deslanoside

    Deacetyllanatoside C; Desacetyllanatoside C

    Na+/K+ ATPase Drug Metabolite Cardiovascular Disease
    Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations .
  • HY-100869A
    MM-589 TFA

    Histone Methyltransferase Cancer
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
  • HY-B0422S
    Nateglinide D5

    A4166 D5; Senaglinide D5

    Potassium Channel Dipeptidyl Peptidase Metabolic Disease
    Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1] [2] .
  • HY-15180
    Buparlisib Hydrochloride

    BKM120 Hydrochloride; NVP-BKM120 Hydrochloride

    PI3K Apoptosis Cancer
    Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
  • HY-16071
    AT13148

    Akt PKA ROCK Ribosomal S6 Kinase (RSK) Cancer
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
  • HY-12532
    Astemizole

    R 43512

    Histamine Receptor Potassium Channel Inflammation/Immunology Endocrinology
    Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.
  • HY-110193
    SPP-86

    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.
  • HY-B0656
    Rabeprazole

    LY307640

    Proton Pump Apoptosis Cancer Inflammation/Immunology
    Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • HY-100490
    Rilmenidine

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cardiovascular Disease
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-N0284
    Esculetin

    PI3K Akt Cancer Inflammation/Immunology
    Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.
  • HY-10197
    Wortmannin

    SL-2052; KY-12420

    PI3K Polo-like Kinase (PLK) Autophagy Cancer
    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
  • HY-13103
    NS 11021

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
  • HY-P0175
    740 Y-P

    740YPDGFR; PDGFR 740Y-P

    PI3K Autophagy Cancer
    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  • HY-B0656A
    Rabeprazole sodium

    LY307640 sodium

    Proton Pump Apoptosis Inflammation/Immunology Cancer
    Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • HY-50694
    Senicapoc

    ICA-17043

    Potassium Channel Others
    Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  • HY-N0392
    Polygalasaponin F

    Toll-like Receptor (TLR) PI3K Akt NF-κB Inflammation/Immunology
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate

    Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride monohydrate is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine hydrochloride monohydrate is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine hydrochloride monohydrate inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension.
  • HY-12059A
    AT7867 dihydrochloride

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-12481
    SAR405

    PI3K Autophagy Cancer
    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
  • HY-N6950
    Hederacolchiside A1

    PI3K Akt mTOR Parasite Apoptosis Cancer Infection
    Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
  • HY-13334
    BGT226 maleate

    NVP-BGT226 maleate

    PI3K mTOR Autophagy Apoptosis Cancer
    BGT226 maleate (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
  • HY-N1967
    Dihydrocurcumin

    Fatty Acid Synthase (FASN) Metabolic Disease
    Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
  • HY-P1565A
    Transdermal Peptide TFA

    TD 1 (peptide) (TFA)

    Na+/K+ ATPase Others
    Transdermal Peptide TFA (TD 1 peptide TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide TFA can enhance the transdermal delivery of many macromolecules.
  • HY-N6843
    Arnicolide D

    Caspase PI3K Akt mTOR STAT Cancer
    Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
  • HY-N5005
    Guanfu base H

    Atisinium chloride

    Parasite Infection
    Guanfu base H (Atisinium chloride) is a diterpenoid alkaloid isolated from Aconitum coreanum and has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 with IC50 values of 4 μM and 3.6 μM, respectively.
  • HY-130307
    Rubrofusarin

    Bacterial Cancer Inflammation/Immunology Neurological Disease
    Rubrofusarin is an orange polyketide pigment from Fusarium graminearum. Rubrofusarin is also an active ingredient of the Cassia species and ameliorates chronic restraint stress (CRS) -induced depressive symptoms through PI3K/Akt signaling. Rubrofusarin has anticancer, antibacterial, and antioxidant effects.
  • HY-13002
    Torin 2

    mTOR DNA-PK Autophagy Apoptosis Cancer
    Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
  • HY-12059
    AT7867

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-N7363
    Isolongifolene

    (-)-Isolongifolene

    Others Cancer Inflammation/Immunology Neurological Disease
    Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-N0314
    Pectolinarin

    Interleukin Related Prostaglandin Receptor NO Synthase Apoptosis Inflammation/Immunology
    Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway.
  • HY-13334A
    BGT226

    NVP-BGT226

    PI3K mTOR Autophagy Cancer
    BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
  • HY-130354
    Dibutyryl-cGMP sodium

    Bt2cGMP sodium

    Potassium Channel Cardiovascular Disease
    Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
  • HY-N4042
    Hirsutenone

    PI3K ERK Cancer Inflammation/Immunology
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
  • HY-116035
    Nimbolide

    NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
  • HY-16585
    VS-5584

    SB2343

    PI3K mTOR Cancer
    VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
  • HY-121246
    Fluorofenidone

    AKF-PD

    Others Inflammation/Immunology
    Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway.
  • HY-123940
    SGC-AAK1-1

    Wnt Cancer
    SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.
  • HY-12868
    Bimiralisib

    PQR309

    PI3K mTOR Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
  • HY-135746
    OR-1896

    Potassium Channel Phosphodiesterase (PDE) Drug Metabolite Cardiovascular Disease
    OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
  • HY-P2266
    SAH-EZH2

    Histone Methyltransferase
    SAH-EZH2 is an EZH2/EPP interaction inhibitor (Kd = 320 nM). SAH-EZH2 suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. SAH-EZH2 arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
  • HY-10220
    SF1126

    PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • HY-114331
    DLK-IN-1

    MAP3K Neurological Disease
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
  • HY-N6790
    Nonactin

    Ammonium ionophore I

    Potassium Channel Mitochondrial Metabolism Bacterial Influenza Virus Apoptosis Antibiotic Cancer Infection
    Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4 +. Nonactin is able to uncouple the oxidative phosphorylation of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin. Nonactin inhibits the surface expression of endogenous HSP60.
  • HY-100421
    CPI-455

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • HY-13440
    AMG 511

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • HY-B0656S
    Rabeprazole D4

    LY307640 D4

    Proton Pump Apoptosis Cancer Inflammation/Immunology
    Rabeprazole D4 (LY307640 D4) is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • HY-124652
    TBK1/IKKε-IN-4

    IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
  • HY-10115
    PI-103

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
  • HY-100764
    YUKA1

    Histone Demethylase Cancer
    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
  • HY-114209
    MRK-740

    Histone Methyltransferase Cancer
    MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM).
  • HY-10115A
    PI-103 Hydrochloride

    PI3K mTOR DNA-PK Autophagy Apoptosis Cancer
    PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
  • HY-15672
    FM19G11

    HIF/HIF Prolyl-Hydroxylase Cancer Neurological Disease
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
  • HY-P1079
    ω-Agatoxin TK

    Calcium Channel Neurological Disease
    ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+ channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.
  • HY-N0678
    Icaritin

    Anhydroicaritin

    Autophagy Apoptosis Cancer
    Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
  • HY-120400
    KDM5-C70

    Histone Demethylase Cancer
    KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
  • HY-10297
    Omipalisib

    GSK2126458; GSK458

    PI3K mTOR Autophagy Cancer
    Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.
  • HY-12037
    Rigosertib sodium

    ON-01910 sodium

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-12596
    JNJ-26489112

    Calcium Channel Sodium Channel Potassium Channel Neurological Disease
    JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
  • HY-50673
    Dactolisib

    BEZ235; NVP-BEZ235

    PI3K mTOR Autophagy Cancer
    Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
  • HY-108573
    P-1075

    Potassium Channel Cardiovascular Disease
    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-N2959
    Brevilin A

    JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
  • HY-121222
    alpha-Bisabolol

    Apoptosis Cancer
    alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
  • HY-112234
    L-Sepiapterin

    Sepiapterin

    Endogenous Metabolite Cancer
    L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression.
  • HY-N2557
    Euphorbia Factor L1

    Apoptosis Cancer Cardiovascular Disease
    Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect.
  • HY-102047
    KDOAM-25

    Histone Demethylase Cancer
    KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-125789
    PF-04753299

    Bacterial Infection
    PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection.
  • HY-110143
    CLP257

    Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
  • HY-102047A
    KDOAM-25 trihydrochloride

    Histone Demethylase Cancer
    KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-13807
    UNC0646

    Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
  • HY-14183
    Vernakalant Hydrochloride

    RSD1235 hydrochloride

    Potassium Channel Cardiovascular Disease
    Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
  • HY-12513
    Samotolisib

    LY3023414

    PI3K DNA-PK mTOR Autophagy Cancer
    Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.
  • HY-125837A
    MS31 trihydrochloride

    Epigenetic Reader Domain Cancer
    MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
  • HY-101562
    GDC-0077

    RG6114

    PI3K Apoptosis Cancer
    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    nAChR Metabolic Disease Inflammation/Immunology Neurological Disease
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
  • HY-123824
    GNE-0439

    Others Neurological Disease
    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-102047B
    KDOAM-25 citrate

    Histone Demethylase Cancer
    KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-N1435
    Oroxin B

    Apoptosis PI3K PTEN Autophagy Cancer
    Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
  • HY-125837
    MS31

    Epigenetic Reader Domain Cancer
    MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.
  • HY-15598
    20-HETE

    20-hydroxy Arachidonic Acid

    Potassium Channel NF-κB NO Synthase Reactive Oxygen Species NADPH Oxidase Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    20-HETE (20-hydroxy Arachidonic Acid) is a CYP450 metabolite and a potent vasoconstrictor. 20-HETE is an endogenous inhibitor of the large-conductance Ca 2+-activated K + channel in renal arterioles. 20-HETE constricts smooth muscles, stimulates smooth muscle proliferation and migration. 20-HETE increases NADPH oxidase, ROS, and NF-κB activity. 20-HETE also inhibits endothelial NO synthase and inhibits apoptosis of pulmonary artery smooth muscle cells.
  • HY-76474
    BAY 61-3606

    Syk Apoptosis Cancer Inflammation/Immunology
    BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • HY-131312
    Mutant IDH1-IN-6

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
  • HY-14985
    BAY 61-3606 dihydrochloride

    Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-N0261
    Aurantio-obtusin

    Others Inflammation/Immunology Cardiovascular Disease
    Aurantio-obtusin is an anthraquinone isolated from Semen Cassiae, with anti-Inflammatory, anti-oxidative, anti-coagulating and anti-hypertension activities. Aurantio-obtusin relaxes systemic arteries through endothelial PI3K/AKT/eNOS-dependent signaling pathway in rats, thus acts as a new potential vasodilator. Aurantio-obtusin inhibits allergic responses in IgE-mediated mast cells and anaphylactic models and is potential for treatment for allergy-related diseases.
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-N2447
    Amarogentin

    AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-123823
    Nitroaspirin

    NCX 4016

    COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 (NSC 697286; SF 1101) is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-112457
    MK-2 Inhibitor III

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM, and is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
  • HY-133028
    CKI-7 free base

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
  • HY-N6742
    Borrelidin

    Treponemycin

    CDK Parasite Apoptosis Antibiotic Infection
    Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin (Treponemycin) is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-19896
    COTI-2

    MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-101508
    GNA002

    Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-N2515
    Ginsenoside Rk1

    NF-κB PI3K JAK Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.