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Pathways Recommended: PI3K/Akt/mTOR
Targets Recommended: Akt

Results for "Akt Modulators" in MCE Product Catalog:

588

Inhibitors & Agonists

13

Screening Libraries

29

Peptides

1

Inhibitory Antibodies

115

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-112148
    AKT-IN-2

    Akt Cancer
    AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1.
  • HY-10249A
    AKT Kinase Inhibitor

    Akt Cancer
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
  • HY-18296
    AKT-IN-1

    Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • 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-50900
    gamma-Secretase Modulators

    Amyloid-β production inhibitor; γ-Secretase Modulators

    Amyloid-β Neurological Disease
    gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease.
  • HY-10721
    PF-AKT400

    Akt protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-10355
    AKT inhibitor VIII

    Akti-1/2

    Akt Apoptosis Cancer Metabolic Disease
    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
  • HY-130988
    Ipatasertib-NH2

    GDC-0068-NH2; RG7440-NH2

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 (HY-133120) to degrade AKT.
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • HY-130987
    Lenalidomide-C9-aldehyde

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041 (HY-133120). INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
  • HY-130985
    9-Decyn-1-ol

    PROTAC Linker Cancer
    9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
  • HY-N2232
    N-​Feruloyloctopamine

    Akt p38 MAPK Cancer
    N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and p38 MAPK.
  • HY-101058
    PD1-PDL1-IN 1

    PD-1/PD-L1 Inflammation/Immunology
    PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator.
  • HY-P1115
    AKTide-2T

    Akt Others
    AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • HY-P1115A
    AKTide-2T TFA

    Akt Others
    AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • 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-117959
    TAK-615

    LPL Receptor Inflammation/Immunology
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
  • 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-114348
    N,N'-Diacetyl-L-cystine

    DiNAC; (Ac-Cys-OH)2

    Others Cardiovascular Disease
    N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-17609
    Difelikefalin

    CR-845; FE-202845

    Opioid Receptor Neurological Disease
    Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
  • HY-15965
    Uprosertib

    GSK2141795

    Akt Cancer
    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15965A
    Uprosertib hydrochloride

    GSK2141795 (hydrochloride)

    Akt Cancer
    Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15431
    Capivasertib

    AZD5363

    Akt Autophagy Cancer
    Capivasertib (AZD5363) is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
  • 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-124600
    NVR 3-778

    HBV Infection
    NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
  • HY-100018
    BAY1125976

    Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, 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-15727
    Afuresertib

    GSK2110183

    Akt PKC ROCK Cancer
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15727A
    Afuresertib hydrochloride

    GSK2110183 hydrochloride

    Akt PKC ROCK Cancer
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-18366A
    RU-SKI 43 hydrochloride

    Hedgehog Cancer
    RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity.
  • HY-18366
    RU-SKI 43

    Hedgehog Cancer
    RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity.
  • HY-113008A
    cis-Urocanic acid

    (Z)-Urocanic acid; cis-UCA

    5-HT Receptor Inflammation/Immunology
    cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-15186
    Ipatasertib

    GDC-0068; RG7440

    Akt Cancer
    Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-15186A
    Ipatasertib dihydrochloride

    GDC-0068 dihydrochloride; RG-7440 dihydrochloride

    Akt Cancer
    Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-10425
    A-443654

    Akt Cancer
    A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
  • 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-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-13757AS
    Tamoxifen-​d5

    ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-19719
    Miransertib

    ARQ-092

    Akt Cancer
    Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
  • 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-16666
    3CAI

    Akt Cancer
    3CAI is a potent and specific AKT1 and AKT2 inhibitor.
  • HY-133120
    INY-03-041

    PROTAC Akt Cancer
    INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-113756A
    Latanoprost acid

    Prostaglandin Receptor Inflammation/Immunology
    Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen activates autophagy and induces apoptosis.
  • HY-111052
    AZD7325

    GABA Receptor Cytochrome P450 Inflammation/Immunology Neurological Disease
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
  • 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-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-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-122913
    Borussertib

    Akt Cancer
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt.
  • HY-108232
    MK-2206

    Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.
  • HY-10249
    GSK-690693

    Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-N0004
    Oridonin

    NSC-250682; Isodonol

    Akt Bacterial Cancer Infection Inflammation/Immunology
    Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
  • HY-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-135671
    AhR modulator-1

    Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR Cancer Endocrinology
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
  • HY-10018
    Toll-like receptor modulator

    Toll-like Receptor (TLR) Inflammation/Immunology
    Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
  • HY-123938
    CYH33

    PI3K Cancer
    CYH33 is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.
  • 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-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-15618
    MK-7622

    M1 receptor modulator

    mAChR Neurological Disease
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
  • HY-102080
    SAFit2

    FKBP Cancer
    SAFit2 is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.
  • 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-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-13254A
    A-674563 hydrochloride

    Akt Cancer
    A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.
  • HY-13254
    A-674563

    Akt Cancer
    A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM.
  • HY-16461
    Solenopsin

    Akt Cardiovascular Disease
    Solenopsin is an ATP-competitive AKT inhibitor with IC50 value of 10 μM .
  • HY-50889
    gamma-secretase modulator 3

    γ-secretase Neurological Disease
    gamma-secretase modulator 3 is a gamma-secretase modulator.
  • HY-15369
    FPA-124

    Akt Apoptosis Cancer
    FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
  • HY-110066
    (Z)-Guggulsterone

    Apoptosis VEGFR Akt Cancer
    Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
  • HY-P0315
    Crosstide

    Akt Others
    Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.
  • 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-135419
    CB2 modulator 1

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia.
  • HY-50162
    GPR120 modulator 1

    GPR120 Metabolic Disease
    GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • HY-50172
    GPR120 modulator 2

    GPR120 Metabolic Disease
    GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • HY-N6905
    Acetylarenobufagin

    HIF/HIF Prolyl-Hydroxylase Cancer
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
  • HY-136006
    (S,R,S)-AHPC-C6-NH2 dihydrochloride

    VH032-C6-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487B
    (S,R,S)-AHPC-C8-NH2

    VH032-C8-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-136006A
    (S,R,S)-AHPC-C6-NH2 hydrochloride

    VH032-C6-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487
    (S,R,S)-AHPC-C8-NH2 dihydrochloride

    VH032-C8-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-133487A
    (S,R,S)-AHPC-C8-NH2 hydrochloride

    VH032-C8-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 hydrochloride (VH032-C8-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 hydrochloride is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-13425
    Deguelin

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

    Akt Autophagy Cancer
    Deguelin, a naturally occurring rotenoid, is a potent PI3K/AKT inhibitor.
  • HY-101625
    Recilisib

    Ex-RAD; ON 01210

    Akt PI3K Cancer
    Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
  • HY-12812
    Autotaxin modulator 1

    Phosphodiesterase (PDE) Others
    Autotaxin modulator 1 is a novel Autotaxin modulator extracted from Patent WO 2014018881 A1.
  • HY-N1505
    Loureirin A

    Akt Cardiovascular Disease
    Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
  • HY-N0371
    Pachymic acid

    3-O-Acetyltumulosic acid

    Akt ERK Cancer
    Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and ERK signaling pathways.
  • HY-112154
    CXCR7 modulator 2

    CXCR Cardiovascular Disease Endocrinology
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-50754
    gamma-secretase modulator 2

    γ-secretase Neurological Disease
    gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.
  • HY-U00135
    Calcium channel-modulator-1

    Calcium Channel Cardiovascular Disease
    Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC50 of 0.8 μM.
  • HY-111996
    Kv3 modulator 1

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.
  • HY-110201
    Estrogen receptor modulator 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
  • HY-U00420
    Opioid receptor modulator 1

    Opioid Receptor Neurological Disease
    Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
  • HY-U00429
    NOT Receptor Modulator 1

    Others Neurological Disease
    NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
  • HY-11005
    BX-912

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
  • HY-10524
    GSK1904529A

    IGF-1R Cancer Endocrinology
    GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
  • 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-107987
    CXCR7 modulator 1

    CXCR Endocrinology
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  • HY-124906
    JAMI1001A

    iGluR Neurological Disease
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
  • HY-13724B
    Pipendoxifene hydrochloride

    Estrogen Receptor/ERR Cancer
    Pipendoxifene hydrochloride is a selective estrogen receptor modulators (SERMs).
  • 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-105272A
    Loreclezole hydrochloride

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-105272
    Loreclezole

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-112699
    AMPA receptor modulator-1

    iGluR Neurological Disease
    AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
  • HY-15673
    KP-23172

    PI3K Akt Cancer
    KP-23172 is a PI3-K/Akt pathway inhibitor extracted from patent US7196083.
  • HY-50909
    Perifosine

    KRX-0401; NSC 639966; D21266

    Akt Autophagy Apoptosis Cancer
    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
  • HY-N2283
    Deltonin

    ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
  • HY-15457
    Triciribine

    API-2; NSC 154020; TCN

    DNA/RNA Synthesis Akt HIV Cancer
    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
  • HY-108714
    NGP555

    γ-secretase Neurological Disease
    NGP555 is a γ-secretase modulator.
  • HY-19832
    SC66

    Akt Apoptosis Cancer
    SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
  • HY-16734A
    Amiselimod hydrochloride

    MT-1303 hydrochloride

    LPL Receptor Cancer
    Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
  • HY-19758A
    Sirtuin modulator 1

    Sirtuin Cancer
    Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
  • HY-103668A
    SSD114 hydrochloride

    GABA Receptor Neurological Disease
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
  • HY-16950
    4-Hydroxytamoxifen

    (Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
  • HY-B0463
    Clomiphene citrate

    Clomifene citrate

    Estrogen Receptor/ERR Endocrinology
    Clomiphene citrate (Clomifene citrate) is a selective estrogen receptor modulator.
  • HY-101216
    Org-26576

    iGluR Neurological Disease
    Org-26576 is a AMPA receptor positive allosteric modulator.
  • HY-16423
    Rapacuronium bromide

    Org 9487

    mAChR Neurological Disease
    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  • HY-14612
    CPPHA

    mGluR Neurological Disease
    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  • HY-112819
    Insulin levels modulator

    Insulin Receptor Metabolic Disease Endocrinology
    Insulin levels modulator could be used to treat diabetes.
  • 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-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-111763
    GPR40/FFAR1 modulator 1

    GPR40 Metabolic Disease
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  • HY-130800
    Cereblon modulator 1

    Ligand for E3 Ligase Apoptosis Cancer Inflammation/Immunology
    Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).
  • HY-114314
    BA-53038B

    HBV Infection
    BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-128581
    γ-Secretase modulator 4

    γ-secretase Neurological Disease
    γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively.
  • HY-111386
    E-7386

    Epigenetic Reader Domain Cancer
    E-7386 is an orally active CBP/beta-catenin modulator.
  • HY-19487
    Ribocil

    Bacterial Infection
    Ribocil is a highly selective chemical modulator of bacterial riboflavin riboswitches.
  • HY-16716
    Basmisanil

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-A0038
    Lasofoxifene Tartrate

    CP-336156

    Estrogen Receptor/ERR Endocrinology
    Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).
  • HY-114530
    LY2452473

    Androgen Receptor Cancer Metabolic Disease
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  • HY-101858
    BQCA

    mAChR Neurological Disease
    BQCA a highly selective allosteric modulator of the M1 mAChR.
  • HY-117291A
    XMD-17-51 Trifluoroacetate

    Others Others
    XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that is able to modulate protein kinases.
  • HY-100186
    GSK-2881078

    Androgen Receptor Neurological Disease
    GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia.
  • HY-18705
    Azoramide

    Apoptosis Endocrinology
    Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
  • HY-101845
    FITM

    mGluR Cancer
    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  • HY-128831
    Kv3 modulator 4

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.
  • HY-18271
    CaMKII-IN-1

    CaMK Autophagy Inflammation/Immunology
    CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.
  • HY-104047
    LM22B-10

    Trk Receptor Akt ERK Neurological Disease
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-16563
    Narciclasine

    Lycoricidinol

    ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-128829
    Kv3 modulator 2

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
  • HY-106182
    TBC3711

    Endothelin Receptor Endocrinology
    TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
  • HY-12505
    CX546

    iGluR Autophagy Neurological Disease
    CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
  • HY-N0273
    Brassinolide

    Brassin lactone

    Apoptosis Cancer
    Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
  • HY-N2371
    27-Hydroxycholesterol

    Estrogen Receptor/ERR LXR Endogenous Metabolite Cancer
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-112788
    ONO-8590580

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • HY-N4182
    Licochalcone E

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
  • HY-N0361
    Dihydrocapsaicin

    TRP Channel Metabolic Disease
    Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.
  • HY-130680
    Syk-IN-3

    Syk Cancer
    Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
  • 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-14383
    RAD140

    Androgen Receptor Endocrinology Cancer
    RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).
  • HY-111453
    AZD7594

    AZ13189620

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
  • HY-101488
    CC-885

    Ligand for E3 Ligase Cancer
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
  • HY-U00178
    Idoxifene

    CB7432

    Estrogen Receptor/ERR Cancer
    Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
  • HY-B1405
    Dehydroisoandrosterone 3-acetate

    Dehydroepiandrosterone 3-acetate; DHEA acetate

    Androgen Receptor Endocrinology Cancer
    Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    Others Cancer
    Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
  • HY-U00339
    H3 receptor-MO-1

    Histamine Receptor Endocrinology
    H3 receptor-MO-1 is a modulator of histamine H3 receptor.
  • HY-124295
    MPT0E028

    HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-N0551
    Wedelolactone

    Caspase Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
  • HY-107457
    AZD-8529

    mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-101093
    PD-1-IN-1

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO2015033299A1, compound example 4. PD-1-IN-1 can be used as immune modulator.
  • HY-100550
    MSDC 0160

    Mitoglitazone; CAY10415

    Insulin Receptor Mitochondrial Metabolism Neurological Disease Endocrinology
    MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
  • 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-113204
    N-Oleoyl glycine

    Endogenous Metabolite Cannabinoid Receptor Akt Metabolic Disease
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
  • HY-P0079
    Neuromedin N

    Neuromedin N (rat, mouse, porcine, canine)

    Dopamine Receptor Neurological Disease
    Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes.
  • HY-N1368B
    (-)-Borneol

    L-Borneol

    GABA Receptor Neurological Disease
    (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
  • HY-10937
    Farampator

    CX-691; Org24448

    iGluR Neurological Disease
    Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.
  • HY-109073
    Rovazolac

    LXR Inflammation/Immunology
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
  • HY-112564
    JNJ-632

    HBV Infection
    JNJ-632 is a hepatitis B virus (HBV) capsid assembly modulator (CAM).
  • HY-15476
    VU 0364439

    mGluR Neurological Disease
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
  • HY-100507
    Avadomide

    CC 122

    E1/E2/E3 Enzyme Apoptosis Cancer Inflammation/Immunology
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-107457A
    AZD-8529 mesylate

    mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-103454
    MPP dihydrochloride

    Estrogen Receptor/ERR Cancer
    MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα.
  • HY-18102A
    GLPG0492 R enantiomer

    Androgen Receptor Neurological Disease
    GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.
  • HY-19559
    JNJ-46778212

    VU 0409551

    mGluR Neurological Disease
    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  • HY-13262
    Lumacaftor

    VX-809; VRT 826809

    CFTR Autophagy Inflammation/Immunology
    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
  • HY-107651
    VU 0365114

    mAChR Others
    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • HY-Y0248A
    Farnesol

    Endogenous Metabolite Bacterial Antibiotic Infection Cancer
    Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
  • HY-11027
    MK-0773

    PF-05314882

    Androgen Receptor Endocrinology
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
  • HY-10932
    Aniracetam

    Ro 13-5057

    nAChR iGluR Neurological Disease
    Aniracetam(Ro 13-5057) is a nootropics and neuroprotective drug, which is selectively modulates the AMPA receptor and nAChR.
  • HY-114775
    RCGD423

    Interleukin Related Inflammation/Immunology Neurological Disease
    RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
  • HY-12023
    Andarine

    GTx-007; S-4

    Androgen Receptor Cancer
    Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.
  • HY-123390
    DB07107

    Bcr-Abl Akt Cancer
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-128830
    Kv3 modulator 3

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
  • HY-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.
  • HY-13058B
    (R)-ADX-47273

    mGluR Neurological Disease
    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  • HY-101291
    Iberdomide

    CC-220

    Ligand for E3 Ligase Apoptosis Inflammation/Immunology Cancer
    Iberdomide (CC-220) is a cereblon (CRBN) modulator with an IC50 value of 60 nM.
  • HY-15255
    Zosuquidar

    LY335979

    P-glycoprotein Cancer
    Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  • HY-109037
    Mavacamten

    MYK461; SAR439152

    Myosin Cardiovascular Disease
    Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
  • HY-18162
    JNJ-42153605

    mGluR Neurological Disease
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
  • HY-19720
    Emixustat

    ACU-4429

    Others Metabolic Disease
    Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
  • HY-16998
    SR2211

    ROR Inflammation/Immunology
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
  • HY-B0005A
    Toremifene

    GTx 006; Z-Toremifene

    Estrogen Receptor/ERR Cancer
    Toremifene (NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-109046
    Tulrampator

    CX-1632

    iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • HY-101746
    GSK376501A

    PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  • HY-101583
    NEO 376

    SPI-376

    5-HT Receptor GABA Receptor Dopamine Receptor Neurological Disease
    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  • HY-15393
    VU 0357121

    mGluR Neurological Disease
    VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.
  • HY-103443
    HKI-357

    EGFR Cancer
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
  • HY-N2110
    Phellopterin

    Others Inflammation/Immunology
    Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
  • HY-N2217
    Rotundic acid

    Akt mTOR p38 MAPK Apoptosis Inflammation/Immunology Cardiovascular Disease Cancer
    Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities.
  • HY-107661
    Arundic Acid

    ONO-2506; (R)-2-Propyloctanoic acid

    Others Neurological Disease
    Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid (ONO-2506) has been developed as a therapeutic agent for stroke and Alzheimer’s disease.
  • 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-16766
    Decoglurant

    RO4995819

    mGluR Neurological Disease
    Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.
  • HY-18292
    ARN2966

    Amyloid-β Neurological Disease
    ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
  • HY-100728
    BMT-145027

    mGluR Neurological Disease
    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  • HY-100298
    Caldaret

    MCC-135

    Na+/Ca2+ Exchanger Cardiovascular Disease
    Caldaret is an intracellular Ca 2+ handling modulator that acts through reverse mode Na +/Ca 2+ exchanger inhibition.
  • HY-17590
    Radafaxine hydrochloride

    GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
  • HY-17030
    Acamprosate calcium

    Calcium N-acetylhomotaurinate

    GABA Receptor Neurological Disease
    Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
  • HY-16950B
    (E)-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    (E)-4-Hydroxytamoxifen, the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
  • HY-B0005
    Toremifene Citrate

    FC 1157a; NK 622

    Estrogen Receptor/ERR Apoptosis Cancer
    Toremifene Citrate(NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  • HY-112282
    BI-1408

    γ-secretase Neurological Disease
    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for 42.
  • HY-111498
    RGX-104

    LXR Cancer Inflammation/Immunology
    RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-19872
    AZD-6280

    GABA Receptor Neurological Disease
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
  • HY-14419
    TCN238

    mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • HY-109011
    Rosiptor

    AQX-1125

    Phosphatase Cancer
    Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
  • HY-122751
    (R)-DNMDP

    Phosphodiesterase (PDE) Cancer
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12).
  • HY-12949
    ML204

    TRP Channel Neurological Disease
    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  • HY-B2121
    6-Methoxy-2-naphthoic acid

    Naproxen impurity O

    iGluR Neurological Disease
    6-Methoxy-2-naphthoic acid is an NMDA receptor modulator extracted from patent WO 2012019106 A2.
  • HY-13058
    ADX-47273

    mGluR Neurological Disease
    ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
  • HY-16728
    Rapastinel

    GLYX-13

    iGluR Neurological Disease
    Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
  • HY-W001692
    Ocinaplon

    DOV 273547

    GABA Receptor Neurological Disease
    Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit.
  • HY-111536
    Mitochonic acid 5

    MA-5

    Mitochondrial Metabolism Cardiovascular Disease
    Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
  • HY-125880
    SBI-553

    Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-112426
    LAU159

    GABA Receptor Neurological Disease
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  • HY-18654
    ADX88178

    mGluR Neurological Disease
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  • HY-119941
    VU0652835

    mGluR Neurological Disease
    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  • HY-101855
    Anle138b

    Others Neurological Disease
    Anle138b is an oligomeric aggregation inhibitor. Anle138b is an oligomer modulator for neurodegenerative diseases such Parkinson's disease.
  • HY-Y0272
    Saccharin

    Bacterial Inflammation/Immunology
    Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
  • HY-N2255
    Crebanine

    Akt Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect.
  • HY-N0427
    Phellodendrine

    Akt NF-κB Inflammation/Immunology
    Phellodendrine, a isoquinoline alkaloid, is one of important characteristic ingredients in the Phellodendri chinensis cortex. phellodendrine is against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway. Phellodendrine has good antioxidant, and anti-inflammatory effect .
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-112633
    SMN-C3

    DNA/RNA Synthesis Others
    SMN-C3 is an orally active SMN2 splicing modulator and has the potential to treat spinal muscular atrophy (SMA).
  • HY-12509
    PEPA

    iGluR Neurological Disease
    PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
  • HY-100084
    Methyl-3β-hydroxycholenate

    ROR Inflammation/Immunology
    Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
  • HY-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-107456
    E6130

    Others Inflammation/Immunology Endocrinology
    E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
  • HY-12152
    PNU-120596

    NSC 216666

    nAChR Neurological Disease
    PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM.
  • HY-14609A
    MPEP

    mGluR Neurological Disease
    MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
  • HY-P1562
    PUMA BH3

    Bcl-2 Family Cancer
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-12157
    VU 0238429

    mAChR Others
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
  • HY-U00013
    Nitroflurbiprofen

    HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen

    COX Cardiovascular Disease
    Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
  • HY-B1494
    Picrotoxinin

    Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors.
  • HY-13574A
    Biricodar

    VX-710

    P-glycoprotein Cancer
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, 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-N6936
    Sennidin A

    HCV Akt GLUT Infection
    Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
  • HY-124958
    NDMC101

    NF-κB Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
  • HY-13288
    Org 27569

    Cannabinoid Receptor Neurological Disease
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
  • HY-15748
    JNJ-40411813

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
  • HY-100366
    Lu AF21934

    mGluR Neurological Disease
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
  • HY-U00366
    S1PR1-MO-1

    LPL Receptor Inflammation/Immunology
    S1PR-MO-1 is the modulator of sphingosine-1-phosphate receptor, used for research of hyperproliferative, inflammatory diseases.
  • HY-15204
    Tonabersat

    SB-220453

    Gap Junction Protein Inflammation/Immunology Neurological Disease
    Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system.
  • HY-16728B
    Rapastinel Trifluoroacetate

    GLYX-13 Trifluoroacetate

    iGluR Neurological Disease
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
  • HY-U00068
    PPARα-MO-1

    PPAR Metabolic Disease
    PPARα-MO-1 is a potent PPARα modulator extracted from patent WO/2004/110982A1, formula I.
  • HY-13277
    IRAK inhibitor 3

    IRAK Inflammation/Immunology
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  • HY-124622
    NNC-0640

    Glucagon Receptor Metabolic Disease
    NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM.
  • HY-116463
    E1R

    Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
  • HY-A0036
    Bazedoxifene acetate

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
  • HY-112920
    TM-25659

    Others Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
  • HY-119751
    Hematein

    Casein Kinase Akt Wnt Apoptosis Cancer
    Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
  • HY-124674A
    CCT365623 hydrochloride

    Monoamine Oxidase EGFR Akt TGF-beta/Smad Cancer
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
  • 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-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-N6872
    Actein

    JNK Akt Apoptosis Autophagy Cancer
    Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
  • 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-119687
    Bifenazate

    GABA Receptor Infection
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor.
  • HY-114269
    (-)-(S)-B-973B

    nAChR Neurological Disease
    (-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.
  • HY-111098
    GSK1702934A

    TRP Channel Cardiovascular Disease
    GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
  • HY-10043
    gamma-secretase modulator 1

    γ-secretase Neurological Disease
    γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-19371
    Lorediplon

    GABA Receptor Neurological Disease
    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
  • HY-18102
    GLPG0492

    Androgen Receptor Others
    GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.
  • HY-112814
    VU6001376

    mGluR Neurological Disease
    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  • HY-119810
    Seletracetam

    Ucb 44212

    Others Neurological Disease
    Seletracetam (Ucb 44212) is an analog of the antiepileptic agent Levetiracetam. Seletracetam is a small molecule SV2A modulator for the research of epilepsy.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-116896
    LY117018

    Estrogen Receptor/ERR Cancer
    LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
  • HY-10454
    Delanzomib

    CEP-18770

    Proteasome Cancer
    Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
  • HY-100409
    PHCCC

    mGluR Cancer
    PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
  • HY-N3755
    Dihydroresveratrol

    Estrogen Receptor/ERR Cancer
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
  • HY-135914
    JBJ-02-112-05

    EGFR Cancer
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFR L858R/T790M.
  • HY-B0789
    SU6656

    Src FAK Akt Cancer
    SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt ERK Autophagy HCV Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
  • HY-W014102
    L-Alanyl-L-glutamine

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations.
  • HY-103035
    BIO-32546

    Phosphodiesterase (PDE) Cancer
    BIO-32546 (example 12b, S-isomer) is an autotaxin (ATX) modulator, extracted from the patent US20170158687A1.
  • HY-129946
    Dopamine D2 receptor antagonist-1

    Dopamine Receptor Neurological Disease
    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-119433
    Asoprisnil

    J867

    Progesterone Receptor Endocrinology
    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-N2370
    24-Hydroxycholesterol

    iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM.
  • HY-U00151
    Dopropidil

    Calcium Channel Cardiovascular Disease
    Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.
  • HY-111498A
    RGX-104 free Acid

    LXR Cancer Inflammation/Immunology
    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • 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-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-13556A
    Arzoxifene hydrochloride

    LY 353381 HCl; SERM 3

    Estrogen Receptor/ERR Cancer
    Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
  • HY-14425
    NB001

    HTS 09836

    Adenylate Cyclase Neurological Disease
    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  • HY-N2487
    5-Hydroxy-7-acetoxyflavone

    Others Cancer
    5-Hydroxy-7-acetoxyflavone, an active natural flavone derivative found in various plant sources, modulates several biological activities.
  • HY-14399
    Itanapraced

    CHF5074; CSP-1103

    γ-secretase Neurological Disease
    Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
  • HY-10043A
    gamma-secretase modulator 1 hydrochloride

    γ-secretase Neurological Disease
    gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-N2032
    Euphorbiasteroid

    AMPK Cancer Infection Metabolic Disease
    Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
  • HY-101363
    1-BCP

    Piperonylic acid piperidide

    iGluR Neurological Disease
    1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
  • HY-120722
    TCH-165

    Proteasome Cancer
    TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
  • HY-N0549
    (-)-α-Pinene

    GABA Receptor Bacterial Virus Protease Endogenous Metabolite Neurological Disease
    (-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
  • HY-P1562A
    PUMA BH3 TFA

    Bcl-2 Family Cancer
    PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-107597
    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
  • 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-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-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-12212
    Omaveloxolone

    RTA 408

    Keap1-Nrf2 STING Apoptosis Cancer Inflammation/Immunology
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
  • HY-14959
    Ulipristal

    CDB-3236; Deacetyl CDB-2914

    Progesterone Receptor Cancer Endocrinology
    Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
  • HY-133684
    N-Tetradecanoyl-L-homoserine lactone

    Bacterial
    N-Tetradecanoyl-L-homoserine lactone is a major chemical modulators of within and between cell communication and regulation. N-Tetradecanoyl-L-homoserine lactone can be used for the study of quorum sensing in vitro.
  • HY-103306
    Ryanodine

    Others Neurological Disease
    Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
  • HY-133555
    mGluR2 antagonist 1

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
  • 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-P2285
    AC 253

    Amyloid-β
    AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
  • HY-N0712
    Typhaneoside

    Autophagy Inflammation/Immunology Cardiovascular Disease
    Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
  • 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-10933
    Ampalex

    CX516; BDP 12; Ampakine CX516

    iGluR Neurological Disease
    Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
  • HY-119165
    GSM-1

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
  • HY-114406
    TD-106

    Ligand for E3 Ligase Cancer
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
  • HY-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-N6935
    Sennidin B

    HCV Akt GLUT Infection Metabolic Disease
    Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
  • 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-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-104066
    Theliatinib

    HMPL-309

    EGFR Cancer
    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
  • HY-15978
    P7C3-A20

    Others Neurological Disease
    P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
  • HY-B0094
    Artemisinin

    Qinghaosu; NSC 369397

    HCV Parasite Akt Ferroptosis Cancer Infection Neurological Disease
    Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective 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-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-126307
    Urolithin B

    NF-κB JNK ERK Akt AMPK Endogenous Metabolite Inflammation/Immunology
    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
  • 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-N2096
    Kavain

    GABA Receptor Neurological Disease
    Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
  • HY-19845A
    Piperidine-MO-1

    Dopamine Receptor Neurological Disease
    Piperidine-MO-1 is a modulator of dopamine receptor extracted from patent WO/2005/121087A1, compound example 2; exhibits an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 (hydrochloride)

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-117965
    Miricorilant

    CORT 118335

    Glucocorticoid Receptor Mineralocorticoid Receptor Endocrinology
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders.
  • HY-P1125
    4-CMTB

    Others Others
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
  • HY-128400
    4'-Methoxychalcone

    PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  • HY-129395
    CC-92480

    E1/E2/E3 Enzyme Apoptosis Cancer
    CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.
  • HY-N3308
    Medicarpin

    Apoptosis Cancer
    Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs.
  • HY-128128
    ASN04421891

    Others Neurological Disease
    ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
  • HY-107409
    GNE 5729

    iGluR Neurological Disease
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC Cancer
    Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • 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-112256
    ACP-105

    Androgen Receptor Inflammation/Immunology
    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  • HY-128770
    LY3154207

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
  • HY-N4157
    Isopteropodine

    mAChR 5-HT Receptor Neurological Disease
    Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors.
  • HY-110278
    ADX71743

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
  • HY-W010104
    L-Methionine sulfoxide

    H-Met(O)-OH

    Endogenous Metabolite Metabolic Disease
    L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.
  • HY-12151
    NS 1738

    NSC 213859

    nAChR Neurological Disease
    NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
  • HY-131181
    LEI-401

    Phospholipase Neurological Disease
    LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.
  • 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-16950A
    (E/Z)-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    (E/Z)-4-Hydroxytamoxifen is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen receptor modulator.
  • HY-108703
    Foliglurax

    PXT002331

    mGluR Neurological Disease
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-108243
    AZD5423

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
  • HY-107902
    RIG-1 modulator 1

    HBV HCV HIV Influenza Virus Infection
    RIG-1 modulator 1 is an anti-viral compound which can be useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV extracted from patent WO 2015172099 A1.
  • HY-112209
    VU0467154

    mAChR Neurological Disease
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    GABA Receptor Neurological Disease
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • HY-105858
    BNC210

    H-Ile-Trp-OH; IW-2143

    nAChR Neurological Disease
    BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
  • HY-10863
    Anandamide

    Cannabinoid Receptor GPR55 Endogenous Metabolite Inflammation/Immunology
    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  • HY-13738A
    Raloxifene hydrochloride

    Keoxifene hydrochloride; LY156758; LY139481 hydrochloride

    Estrogen Receptor/ERR Autophagy Endocrinology Cancer
    Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
  • 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-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • 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-12795
    Vps34-IN-1

    PI3K Autophagy Cancer
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
  • HY-120530
    JNJ-46281222

    mGluR Neurological Disease
    JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
  • HY-103040
    Zuranolone

    GABA Receptor Neurological Disease
    Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-108337
    GNE-0723

    iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
  • HY-125740
    Malvidin-3-glucoside chloride

    Malvidin-3-O-glucoside chloride; Oenin chloride

    Others Inflammation/Immunology
    Malvidin-3-glucoside chloride (Malvidin-3-O-glucoside chloride), a major wine anthocyanin, is effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation.
  • HY-128677
    NCC007

    Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-103575A
    MFZ 10-7 hydrochloride

    mGluR Neurological Disease
    MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
  • HY-B2158
    Chlorotrianisene

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • HY-124867
    D3-βArr

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  • HY-129527
    GNE-9278

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
  • HY-107198
    (2S)-6-Prenylnaringenin

    GABA Receptor Neurological Disease
    (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.
  • HY-108710
    VU0650786

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-17499
    EGFR-IN-12

    EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-15244
    Alpelisib

    BYL-719

    PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-135805
    JBJ-04-125-02

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-10253
    AG1024

    Tyrphostin AG 1024

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of insulin receptor (IR; IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • HY-101364A
    CHPG sodium salt

    mGluR NF-κB ERK Akt Inflammation/Immunology Neurological Disease
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
  • HY-N7110
    6-Hydroxyflavone

    Others Inflammation/Immunology
    6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
  • HY-101364
    CHPG

    mGluR NF-κB ERK Akt Inflammation/Immunology Cardiovascular Disease
    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
  • HY-128932
    Cefminox sodium

    MT-141

    Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • HY-10971
    Alisertib

    MLN 8237

    Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-N2585
    Isodeoxyelephantopin

    Reactive Oxygen Species NF-κB Autophagy Cancer
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
  • HY-108703A
    Foliglurax monohydrochloride

    PXT002331 (monohydrochloride)

    mGluR Neurological Disease
    Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-12324
    SB269652

    Dopamine Receptor Neurological Disease
    SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  • HY-120012
    AZD9567

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
  • HY-101792A
    RG7800 hydrochloride

    RO6885247 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.
  • HY-15731
    Estetrol

    Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
  • HY-101281
    VU 6008667

    mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
  • HY-13738
    Raloxifene

    Keoxifene; LY156758 free base; LY139481

    Estrogen Receptor/ERR Cancer
    Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-B1837
    Cyfluthrin

    Sodium Channel Infection
    Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
  • HY-12508
    CMPDA

    iGluR Neurological Disease
    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
  • HY-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
  • HY-13963
    ZCL278

    Ras Cancer
    ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
  • HY-111772
    Elexacaftor

    VX-445

    CFTR Autophagy Others
    Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
  • HY-N4180
    Pennogenin 3-O-beta-chacotrioside

    Autophagy Cancer
    Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
  • HY-119332
    3-Keto petromyzonol

    Others Endocrinology
    3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey.
  • HY-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-107091
    Aspartyl-alanyl-diketopiperazine

    DA-DKP

    Others Inflammation/Immunology
    Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
  • HY-135585
    LY88074

    Others Endocrinology
    LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
  • HY-122190
    TAK-071

    mAChR Neurological Disease
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  • HY-16508
    Ulipristal acetate

    CDB-2914

    Progesterone Receptor Autophagy Endocrinology Cancer
    Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
  • HY-11048
    NS11394

    GABA Receptor Neurological Disease
    NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
  • HY-W011100
    Cyclofenil

    Estrogen Receptor/ERR Influenza Virus Infection Endocrinology
    Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
  • HY-100932
    ML-9

    Myosin Cancer
    ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • 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-129636A
    GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • HY-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-123268
    Ro 363

    Adrenergic Receptor Cardiovascular Disease
    Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-N0029
    Forsythoside B

    TNF Receptor NF-κB Inflammation/Immunology
    Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
  • HY-114739
    MA-0204

    PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-108523
    LG100754

    UVI 2112

    RAR/RXR Metabolic Disease
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
  • HY-105296
    Blarcamesine

    AVex-73; AE-37

    Sigma Receptor mAChR
    Blarcamesine (AVex-73;AE-37) is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
  • HY-136151
    UNC10217938A

    Others Others
    UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
  • HY-135572
    TLX agonist 1

    Others Cancer Neurological Disease
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-116819
    VU0453379

    Glucagon Receptor Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-13065
    Isobavachalcone

    Corylifolinin; Isobacachalcone

    Akt Reactive Oxygen Species Apoptosis Autophagy Cancer
    Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
  • HY-12037A
    Rigosertib

    ON-01910

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-10230S
    Midostaurin-D5

    PKC412-D5; CGP 41251-D5

    Others Cancer
    Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-13072
    Cenisertib

    AS-703569; R-763

    Aurora Kinase Bcr-Abl Akt STAT FLT3 Cancer
    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
  • HY-N2259
    Curcumenol

    (+)-Curcumenol

    Cytochrome P450 Cancer Inflammation/Immunology Neurological Disease
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
  • 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-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-19356A
    Didesmethylrocaglamide

    Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.
  • HY-120327
    KY-226

    Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Cancer
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
  • HY-18719D
    Endoxifen E-isomer

    E-Endoxifen

    Estrogen Receptor/ERR Cancer
    Endoxifen E-isomer is the E-isomer of (Z)-Endoxifen. (Z)-Endoxifen, an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than Tamoxifen.
  • HY-100290
    5-HT1A modulator 1

    5-HT Receptor Neurological Disease
    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  • HY-113066
    Guanosine 5'-diphosphate

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-116463D
    (Rac)-E1R

    Sigma Receptor Neurological Disease
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-14569
    CDPPB

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
  • HY-B0719
    Ingenol Mebutate

    Ingenol 3-angelate; PEP005

    PKC Cancer Inflammation/Immunology
    Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
  • 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-W008947
    SEW​2871

    LPL Receptor Inflammation/Immunology Neurological Disease
    SEW2871 is a highly selective, orally active S1P1 agonist with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood and has therapeutic implications in contexts of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
  • HY-100237
    SZL P1-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • 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-N0107
    Cyclovirobuxine D

    Apoptosis Autophagy mTOR Akt Cardiovascular Disease
    Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction.
  • HY-P1222
    LL-37, Human

    Bacterial Infection
    LL-37, Human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human could help protect the cornea from infection and modulates wound healing.
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-107734
    L 152804

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  • HY-121149
    Droloxifene

    3-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
  • HY-115467
    MitoBloCK-10

    Others Metabolic Disease
    MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
  • HY-N0513
    Loganic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
  • HY-128584
    VU6005806

    AZN-00016130

    mAChR Neurological Disease
    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
  • HY-P1303
    CART(62-76)(human,rat)

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • HY-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU 0361737 (ML-128) is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
  • HY-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-123956
    HG-12-6

    IRAK Inflammation/Immunology
    HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
  • HY-N6694
    4-​Bromo A23187

    Calcium Channel Bacterial Apoptosis Antibiotic Cancer Infection
    4-Bromo A23187 is a halogenated analog of the highly selective calcium ionophore A-23187. 4-Bromo A23187,a calcium modulator, induces apoptosis in different cells, including HL-60 cells.
  • HY-106901A
    Asoxime dichloride

    HI-6

    nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • HY-100932A
    ML-9 Free Base

    Myosin Cancer
    ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • 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-N0265
    Asperosaponin VI

    Caspase Cardiovascular Disease
    Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway. Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB.
  • HY-122487
    Troriluzole

    BHV-4157

    Others Neurological Disease
    Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
  • HY-110155A
    (Rac)-LM11A-31 dihydrochloride

    Others Neurological Disease
    (Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-P1222A
    LL-37, Human TFA

    Bacterial Infection
    LL-37, Human TFA is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human TFA could help protect the cornea from infection and modulates wound healing.
  • HY-117977
    FCPR03

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects.
  • HY-N0322
    Cholesterol

    Estrogen Receptor/ERR Endogenous Metabolite Metabolic Disease
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-126145
    S1PR1 modulator 1

    LPL Receptor Inflammation/Immunology
    S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.
  • HY-P1303A
    CART(62-76)(human,rat) TFA

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • HY-N2787
    8-​Prenylnaringenin

    Apoptosis Cancer
    8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
  • 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-12150
    CCMI

    nAChR Neurological Disease
    CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
  • HY-P1397
    RVD-Hpα

    Cannabinoid Receptor
    RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-14417B
    VU0155041 sodium

    mGluR Neurological Disease
    VU0155041 sodium is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 sodium is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site.
  • HY-N0751
    Scutellarin

    STAT Akt HIV Cancer Infection
    Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
  • 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-129636
    (E)-GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    (E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • HY-14611
    3,3'-Difluorobenzaldazine

    DFB

    mGluR Neurological Disease
    3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range.
  • HY-B0723S
    Ospemifene D4

    FC-1271a D4

    Estrogen Receptor/ERR Cancer
    Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
  • HY-120789
    PF-06648671

    γ-secretase Neurological Disease
    PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
  • 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-117639
    AUT1

    Potassium Channel Cancer
    AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
  • HY-122590
    Glabrescione B

    Gli Cancer
    Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-124614
    GLP-26

    HBV Infection
    GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM. GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
  • HY-110279
    Ogerin

    Others Neurological Disease
    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
  • HY-104037
    Cintirorgon

    LYC-55716

    ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • HY-135909
    TH1217

    ZINC1775962367

    SARS-CoV Cancer Infection
    TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
  • HY-N0313
    Euphol

    Endogenous Metabolite MAGL Inflammation/Immunology
    Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
  • HY-P1397A
    RVD-Hpα TFA

    Cannabinoid Receptor
    RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • 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-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-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-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-P2076
    Dusquetide

    SGX942

    Bacterial Cancer Infection
    Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one

    THDOC

    GABA Receptor
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • 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-119695A
    Simvastatin acid ammonium

    Tenivastatin ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-P1216
    HS014

    Melanocortin Receptor Neurological Disease
    HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
  • HY-10016
    E 2012

    γ-secretase Neurological Disease
    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
  • HY-116463B
    (2S,3S)-E1R

    Sigma Receptor Neurological Disease
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-116463A
    (2R,3S)-E1R

    Sigma Receptor Neurological Disease
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-116463C
    (2R,3R)-E1R

    Sigma Receptor Neurological Disease
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-P2076A
    Dusquetide TFA

    SGX942 TFA

    Bacterial Cancer Infection
    Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-W011733
    Tulobuterol hydrochloride

    C-78

    Adrenergic Receptor Influenza Virus Antibiotic Infection Endocrinology Inflammation/Immunology
    Tulobuterol hydrochloride (C-78) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol hydrochloride is also a sympathomimetic agent used as a transdermal patch, increases normal diaphragm muscle strength. Tulobuterol hydrochloride inhibit rhinovirus replication and modulate airway inflammation.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-118342
    PQCA

    mAChR Neurological Disease
    PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
  • HY-B2163
    Astaxanthin

    PPAR Reactive Oxygen Species Cancer Cardiovascular Disease
    Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
  • HY-106225
    Rotigaptide

    ZP123

    Gap Junction Protein Cardiovascular Disease
    Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
  • HY-102070
    NS13001

    Potassium Channel Neurological Disease
    NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
  • 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-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-P1216A
    HS014 TFA

    Melanocortin Receptor Neurological Disease
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
  • HY-131337
    RhlR antagonist 1

    Bacterial Infection
    RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections.
  • HY-B1640
    Ethacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-130609
    Aβ42-IN-1

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • HY-P1075
    CALP3

    Calcium Channel Cancer Neurological Disease
    CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • 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-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-128895
    NQO1 activator 1

    Others Metabolic Disease
    NQO1 activator 1 is an orally available NAD + modulator. It reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD + levels via NADH oxidation. Elevated NAD + levels triggers the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts.
  • HY-111751
    JNJ-61432059

    iGluR Neurological Disease
    JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.
  • HY-N2499
    Dehydrotumulosic acid

    Others Metabolic Disease
    Dehydrotumulosic acid, one of the effective constituents of Poria cocos, was isolated from the chloroform-soluble material of ethanol extract of the fungus. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body.
  • HY-19620
    Branaplam

    LMI070; NVS-SM1

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-12355
    Siponimod

    BAF-312

    LPL Receptor Others
    Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis.
  • HY-121618
    α-Thujone

    GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • 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-P1075A
    CALP3 TFA

    Calcium Channel Cancer Neurological Disease
    CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-13456
    LY-404187

    iGluR Neurological Disease
    LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
  • HY-17600S
    Acalabrutinib D4

    ACP-196 D4

    Btk Cancer
    Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.
  • HY-17600
    Acalabrutinib

    ACP-196

    Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-120355A
    AP14145 hydrochloride

    Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
  • HY-12700
    RO5256390

    Others Neurological Disease
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
  • HY-105231
    Bryostatin 1

    PKC HIV Cancer Infection Inflammation/Immunology Neurological Disease
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
  • HY-P0063
    Copper tripeptide

    GHK-Cu

    Endogenous Metabolite Inflammation/Immunology
    Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
  • HY-117482
    BPN-15606

    γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-135276
    Targaprimir-96

    MicroRNA Apoptosis Cancer
    Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-N0226
    Epiberberine

    AChE Beta-secretase Metabolic Disease Neurological Disease
    Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
  • HY-N0226A
    Epiberberine chloride

    AChE Beta-secretase Reactive Oxygen Species Metabolic Disease Neurological Disease
    Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
  • HY-P1218
    Phrixotoxin 3

    Sodium Channel Neurological Disease
    Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-100588
    VU0364770

    mGluR Neurological Disease
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-110155
    LM11A-31 dihydrochloride

    Others Neurological Disease
    LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
  • HY-P1218A
    Phrixotoxin 3 TFA

    Sodium Channel Neurological Disease
    Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-117482A
    BPN-15606 besylate

    γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-100588A
    VU0364770 hydrochloride

    mGluR Neurological Disease
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-100991
    FG 7142

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
  • HY-135276A
    Targaprimir-96 TFA

    MicroRNA Apoptosis Cancer
    Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • 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.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF3

    Akt NF-κB MEK ERK Cancer
    Theaflavin 3,3'-digallate (TF3), the typical pigment in black tea, is a good antitumor agent. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-N3387
    Licoricidin

    Apoptosis NF-κB Akt MMP Cancer Inflammation/Immunology
    Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer. Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect. Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations.
  • HY-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 has the potential for epilepsy.
  • HY-12403
    Angiotensin (1-7)

    Ang-(1-7)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease Endocrinology
    Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
  • HY-112608
    CHMFL-PI3KD-317

    PI3K Cancer
    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
  • HY-109112
    Brilaroxazine

    RP5063

    Dopamine Receptor 5-HT Receptor Inflammation/Immunology Neurological Disease
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.