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Results for "Ang (1-25) Inhibitors" in MCE Product Catalog:

110

Inhibitors & Agonists

9

Peptides

15

Natural
Products

3

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-120079
    MSN-125

    Bcl-2 Family Cancer
    MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
  • HY-133739
    NBD-125

    RAR/RXR Cancer
    NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
  • HY-100576
    NH125

    CaMK Autophagy Bacterial Fungal Virus Protease Cancer
    NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with an IC50 of 60 nM for eEF-2K.
  • HY-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-W016586
    Acivicin

    AT-125; U-42126

    Parasite Cancer Infection
    Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
  • HY-14452
    Fatostatin

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-15778A
    AVE 0991 sodium salt

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM.
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-10559
    Nelotanserin

    APD125

    5-HT Receptor Cancer Neurological Disease
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
  • 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-90005
    Etravirine

    R165335; TMC125

    Reverse Transcriptase HIV Infection
    Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-15320
    NBI-74330

    CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  • HY-12053A
    Vinorelbine ditartrate

    KW-2307; Nor-5'-anhydrovinblastine ditartrate

    Microtubule/Tubulin Autophagy Cancer
    Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
  • HY-12053
    Vinorelbine

    KW-2307 base

    Microtubule/Tubulin Autophagy Cancer
    Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
  • HY-10002
    Calcitriol

    1,25-Dihydroxyvitamin D3

    VD/VDR Endogenous Metabolite Cancer
    Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.
  • HY-P1533
    CRF, bovine

    Corticotropin Releasing Factor bovine

    CRFR Inflammation/Immunology Endocrinology
    CRF, bovine is a potent agonist of CRF receptor, and displaces [ 125I-Tyr]ovine CRF with a Ki of 3.52 nM.
  • HY-P1533A
    CRF, bovine TFA

    Corticotropin Releasing Factor bovine TFA

    CRFR Inflammation/Immunology Endocrinology
    CRF, bovine (TFA) is a potent agonist of CRF receptor, and displaces [ 125I-Tyr]ovine CRF with a Ki of 3.52 nM.
  • HY-16711
    SB225002

    CXCR Inflammation/Immunology Endocrinology Cancer
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
  • HY-13772
    Valrubicin

    AD-32

    PKC Cancer Inflammation/Immunology
    Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
  • HY-13955
    Telmisartan

    BIBR 277

    Angiotensin Receptor Autophagy Cardiovascular Disease Endocrinology
    Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
  • HY-100183
    GSK2239633A

    CCR Inflammation/Immunology Endocrinology
    GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [ 125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.
  • HY-P1016A
    BQ-3020 TFA

    Endothelin Receptor Cardiovascular Disease Endocrinology
    BQ-3020 (TFA) is a selective agonist of ETB receptor, inhibits [ 125I]ET-1 binding to ETB receptor with an IC50 of 0.2 nM in cerebellum, and causes vasoconstriction.
  • HY-130704
    Isotachysterol 3

    Calcium Channel Metabolic Disease
    Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats.
  • HY-P1104A
    FC131 TFA

    CXCR HIV Infection
    FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
  • HY-107568
    Iodophenpropit dihydrobromide

    Histamine Receptor Inflammation/Immunology
    Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM).
  • HY-19529
    Ro 46-2005

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
  • HY-16293
    Lurbinectedin

    PM01183

    DNA Alkylator/Crosslinker DNA/RNA Synthesis Cancer
    Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
  • HY-13293
    Impurity C of Calcitriol

    VD/VDR Cancer
    Impurity C of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-13292
    Impurity B of Calcitriol

    1β,25-Dihydroxyvitamin-D3; 1-Epicalcitriol

    VD/VDR Cancer
    Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-112274
    M443

    Others Cancer
    M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.
  • HY-76814
    Calcitriol D6

    VD/VDR Metabolic Disease
    Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  • HY-100219
    CB1151

    VD/VDR Cancer
    CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
  • HY-102059
    MOZ-IN-2

    Histone Acetyltransferase Cancer
    MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC50 of 125 μM.
  • HY-P1104
    FC131

    CXCR HIV Infection
    FC131 TFA 是一种 CXCR4 拮抗剂,抑制 [ 125I]-SDF-1 与 CXCR4 结合,IC50 值为 4.5 nM。FC131 TFA 具有抗 HIV 的活性。
  • HY-19768
    Danirixin

    GSK1325756

    CXCR Inflammation/Immunology Endocrinology
    Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
  • HY-15526
    PSI-697

    P-Selectin Inhibitor

    Others Cancer
    PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM.
  • HY-N6679
    (R)-10,11-Dehydrocurvularin

    Others Cancer
    (R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines with a mean IC50 value of 1.25 µM.
  • HY-76915
    24, 25-Dihydroxy VD3

    VD/VDR Endogenous Metabolite Metabolic Disease
    24, 25-Dihydroxy VD3 is a compound which is closely related to 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.
  • HY-101465
    AK-1

    Sirtuin Neurological Disease
    AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM.
  • HY-101609
    Lesopitron dihydrochloride

    E4424

    5-HT Receptor Neurological Disease
    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-A0020
    Eldecalcitol

    ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3

    VD/VDR Metabolic Disease
    Eldecalcitol (ED-71) is an orally active analogue of active vitamin D used in the treatment of osteoporosis. Eldecalcitol (ED-71) possesses a strong inhibitory effect on bone resorption and causes a significant increase in bone mineral density.
  • HY-90005S
    Etravirine D4

    TMC-125 D4; R-165335 D4

    Reverse Transcriptase HIV Infection
    Etravirine D4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-50101A
    Mavorixafor trihydrochloride

    AMD-070 trihydrochloride

    CXCR HIV Infection Endocrinology
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-128780
    SPR206

    Bacterial Cancer Infection
    SPR206 is a polymyxin analogue and an important class of antibiotic for the treatment of bacterial infections due to multidrug resistant Gram-negative pathogen. The MIC values of SPR206 against Pseudomonas aeruginosa Pa14 (MIC value of for Pa14) and Acinetobacter baumannii NCTC13301 are 0.125 mg/L and 0.125 mg/L, respectively.
  • HY-121071
    Ascamycin

    Bacterial Nucleoside Antimetabolite/Analog Infection
    Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces sp. JCM9888. Ascamycin has a selective antibacterial activity against Xanthomonas species with MIC values of 0.4 μg/mL, 12.5 μg/mL and 12.5 μg/mL for Xanthomonas citri, Xanthomonas oryzae and Mycobacterium phlei, respectively.
  • HY-126246
    CDC25B-IN-1

    Phosphatase Cancer
    CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
  • HY-50101
    Mavorixafor

    AMD-070

    CXCR HIV Infection Endocrinology
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-15698A
    CRT0066101 dihydrochloride

    PKD Cancer
    CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-12624
    ON123300

    CDK Cancer
    ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.
  • HY-P0216
    A 779

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
  • HY-12060
    KRN-633

    VEGFR Cancer
    KRN-633 is a potent VEGFR inhibitor with IC50s of 170, 160 and 125 nM for VEGFR1, VEGFR2 and VEGFR3, respectively.
  • HY-N3139
    Ombuin

    Bacterial Infection
    Ombuin, isolated from Zanthoxylum armatum, displays broad spectrum antibacterial effect with MIC ranges from 125 to 500 μg/mL.
  • HY-100891
    CD80-IN-3

    Others Inflammation/Immunology
    CD80-IN-3, a potent CD80 inhibitor, inhibits CD80/CD28 interaction with an EC50 of 630 nM and a Kd of 125 nM.
  • HY-N0060
    Ferulic acid

    Coniferic acid

    FGFR Endogenous Metabolite Cancer
    Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-N0060A
    Ferulic acid sodium

    Coniferic acid sodium

    FGFR Endogenous Metabolite Reactive Oxygen Species Cardiovascular Disease Cancer
    Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-N2326
    (±)-Anatoxin A fumarate

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
  • HY-135283
    ABT-546

    A-216546

    Endothelin Receptor Endocrinology Cardiovascular Disease
    ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
  • HY-108488
    KB SRC 4

    Src Cancer
    KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
  • HY-14850
    Sograzepide

    Netazepide; YF 476; YM-220

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
  • HY-13962
    SGI-1027

    DNA Methyltransferase Apoptosis Cancer
    SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
  • HY-108543
    NSC 95397

    Phosphatase Apoptosis Cancer
    NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
  • HY-108421
    Xinjiachalcone A

    Bacterial Infection
    Xinjiachalcone A is an active principle of Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori, with MIC values ranged from 12.5 to 50 µM for seventeen H. pylori strains.
  • HY-10015
    PAP-1

    5-(4-Phenoxybutoxy)psoralen

    Potassium Channel Inflammation/Immunology
    PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
  • HY-B0117
    Tigecycline

    GAR-936

    Bacterial Autophagy Antibiotic Infection Cancer
    Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
  • HY-B0117A
    Tigecycline hydrochloride

    GAR-936 hydrochloride

    Bacterial Autophagy Antibiotic Infection
    Tigecycline hydrochloride (GAR-936 hydrochloride) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
  • 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-U00326
    PI3Kα/mTOR-IN-1

    PI3K mTOR Cancer
    PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
  • HY-B0117B
    Tigecycline mesylate

    GAR-936 mesylate

    Bacterial Autophagy Antibiotic Infection
    Tigecycline mesylate (GAR-936 mesylate) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
  • HY-10704
    PTP1B-IN-1

    PTP1B inhibitor

    Phosphatase Metabolic Disease
    PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
  • HY-B0117C
    Tigecycline tetramesylate

    GAR-936 tetramesylate

    Bacterial Autophagy Antibiotic Infection Cancer
    Tigecycline tetramesylate (GAR-936 tetramesylate) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
  • HY-114818
    4-(tert-Butyl)-benzhydroxamic Acid

    Bacterial Infection
    4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively. 4-(tert-Butyl)-benzhydroxamic Acid reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM.
  • HY-103353
    SID 26681509

    Cathepsin Parasite Cancer Infection
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
  • HY-111139
    MS417

    GTPL7512

    Epigenetic Reader Domain HIV Infection Inflammation/Immunology
    MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
  • HY-B0793
    AZ-5104

    EGFR Cancer
    AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
  • HY-17593
    Solithromycin

    CEM-101; OP-1068

    Bacterial Antibiotic Infection
    Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis.
  • HY-128772
    XPC-6444

    Sodium Channel Neurological Disease
    XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.
  • HY-128773
    MRL-494

    Bacterial Infection
    MRL-494 is an antibacterial agent and is a small-molecule inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.
  • HY-P1236
    Atrial Natriuretic Peptide (ANP) (1-28), rat

    Atrial natriuretic factor (1-28) (rat)

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-P1236A
    Atrial Natriuretic Peptide (ANP) (1-28), rat TFA

    Atrial natriuretic factor (1-28) (rat) TFA

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Atrial Natriuretic Peptide (ANP) (1-28), rat (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-106994
    Nebentan free base

    YM598 free base

    Endothelin Receptor Inflammation/Immunology Cardiovascular Disease
    Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
  • HY-101189
    JNJ-39758979

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
  • HY-101189B
    JNJ-39758979 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-135646
    Eleutheroside B1

    Influenza Virus Infection Inflammation/Immunology
    Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities.
  • HY-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
  • HY-131347
    PD-1/PD-L1-IN-NP19

    PD-1/PD-L1 Cancer Inflammation/Immunology
    PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-19373
    RWJ-445167

    3DP-10017

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

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-13948A
    Angiotensin II human acetate

    Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis.
  • HY-135795
    1-Cyclohexyl-3-dodecyl urea

    CDU; N-Cyclohexyl-N-dodecyl urea; NCND

    Epoxide Hydrolase Metabolic Disease Cardiovascular Disease
    1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.
  • HY-135813
    LtaS-IN-1

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

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-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-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-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-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-N0515
    Ophiopogonin D

    PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-P0117
    Tat-NR2B9c

    Tat-NR2Bct; NA-1

    iGluR NO Synthase Neurological Disease
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120944
    BAY-7598

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