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Targets Recommended: BCRP P-glycoprotein
Results for "

resistance

" in MCE Product Catalog:

167

Inhibitors & Agonists

6

Screening Libraries

1

Dye Reagents

4

Peptides

49

Natural
Products

3

Recombinant Proteins

8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-N9511
    Jacobine N-oxide

    Others Others
    Jacobine N-oxide, an N-oxide of Jacobine which is a pyrrolizidine alkaloid, can be found in Senecio hybrids that has thrips resistance.
  • HY-106681
    Lagosin

    Fungichromin; Pentamycin; Cogomycin

    Antibiotic Fungal Cancer
    Lagosin (Fungichromin) is a polyene macrolide antibiotic. Lagosin has demonstrated broad-spectrum antifungal activity and is impervious to drug resistance.
  • HY-136217
    PU 23

    Others Cancer
    PU 23 is a non-carboxylic multidrug resistance protein 4 (MRP4) inhibitor as an active agent reducing resistance to anticancer agent 6-Mercaptopurine.
  • HY-107636
    DC_AC50

    Apoptosis Cancer
    DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). Inhibiting intracellular copper chaperones as a means of reducing/preventing acquired chemotherapy resistance.
  • HY-N1995
    Methylswertianin

    Others Metabolic Disease
    Methylswertianin is an active constituent in Swertia punicea Hemsl, with anti-diabetic effect. Methylswertianin can abates type-2 diabetes, likely via the improvement of insulin resistance (IR).
  • HY-N7698B
    Hexa-N-acetylchitohexaose

    Others Cancer Inflammation/Immunology
    Hexa-N-acetylchitohexaose is an inducer of disease resistance in crop plants, which could elicit an increase of lignification-related and antioxidative enzymes in soybean plants. Hexa-N-acetylchitohexaose is a substrate of lysozyme. Hexa-N-acetylchitohexaose shows antitumor effect.
  • HY-B1815
    Xanthinol Nicotinate

    Xanthinol Niacinate

    Others Cardiovascular Disease
    Xanthinol Nicotinate (Xanthinol Niacinate), a vasodilator, can act directly on the smooth muscle of small arteries and capillaries. Xanthinol Nicotinate expands blood vessels, improves blood rheology and reduces peripheral vascular resistance.
  • HY-106690
    Centhaquin

    Centhaquine; PMZ-2010

    Others Inflammation/Immunology Cardiovascular Disease
    Centhaquine (Centhaquin; PMZ-2010) is a novel agent has the potential for treatment of  haemorrhagic shock. Centhaquine (Centhaquin; PMZ-2010) can augment cardiac output, reduce systemic vascular resistance in haemorrhagic models.
  • HY-77641
    Cinnamoylglycine

    Endogenous Metabolite Metabolic Disease
    Cinnamoylglycine is a glycine conjugate of cinnamic acid and a urinary metabolite in human. Cinnamoylglycine is used as a potential urinary biomarker indicating intact or disrupted colonization resistance during and after antibiotic treatment.
  • HY-103460
    IRL 2500

    Endothelin Receptor Cardiovascular Disease
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
  • HY-N1419
    Vaccarin

    AMPK Metabolic Disease
    Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
  • HY-B0947
    Sulfanitran

    Bacterial Infection
    Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
  • HY-N8393
    Ascr#18

    Bacterial Fungal Infection
    Ascr#18, an ascaroside, is a hormone of nematodes. Ascr#18 is expressed during nematode development. Ascr#18 increases resistance in Arabidopsis, tomato, potato and barley to viral, bacterial, oomycete, fungal and nematode infections.
  • HY-107096
    CH-0793076

    TP3076

    Topoisomerase Cancer
    CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
  • HY-107096B
    CH-0793076 TFA

    TP3076 TFA

    Topoisomerase Cancer
    CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
  • HY-N8188
    Dehydrojuncusol

    HCV HCV Protease Infection
    Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM).
  • HY-N7378A
    N-Hydroxypipecolic acid potassium

    1-Hydroxy-2-piperidinecarboxylic acid potassium; NHP potassium

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid potassium (1-Hydroxy-2-piperidinecarboxylic acid potassium), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid potassium accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid potassium induces SAR to bacterial and oomycete infection.
  • HY-N7378
    N-Hydroxypipecolic acid

    1-Hydroxy-2-piperidinecarboxylic acid; NHP

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid (1-Hydroxy-2-piperidinecarboxylic acid), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid induces SAR to bacterial and oomycete infection.
  • HY-139696
    AKR1B10-IN-1

    Aldose Reductase Cancer
    AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells.
  • HY-W062216
    2-Aminoimidazole

    Bacterial Arginase Infection
    2-Aminoimidazole is a potent antibiofilm agent that can be used as an adjuvant to antimicrobial. 2-aminoimidazoles disrupts the ability of bacteria to protect themselves by inhibiting biofilm formation and genetically-encoded antibiotic resistance traits. 2-Aminoimidazole is also a weak noncompetitive inhibitor of human arginase I with a Ki of 3.6 mM.
  • HY-19642
    Glesatinib

    MGCD265

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-N7073
    Silymarin

    SARS-CoV Cancer Infection Inflammation/Immunology Neurological Disease
    Silymarin is an extract of the milk thistle (Silybum marianum). Silymarin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance. Silymarin, a food-derived antiviral molecule, is an effective SARS-CoV-2 main protease (M pro) inhibitor. Silymarin has the chemopreventive effect on hepatocellular carcinoma (HCC). Silymarin has the potential for COVID-19 research.
  • HY-10574
    Rilpivirine

    R278474; TMC278; DB08864

    HIV Reverse Transcriptase Infection
    Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV.
  • HY-12333
    G-749

    FLT3 Apoptosis Cancer
    G-749 is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. G-749 can be used for the research of drug resistance for acute myeloid leukemia (AML).
  • HY-B0362A
    Phentolamine mesylate

    Phentolamine methanesulfonate

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
  • HY-N1423
    Glycocholic acid

    Endogenous Metabolite Cancer
    Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-101595
    RPH-2823

    Others Others
    RPH-2823, a basic triamterene derivative, induces a dose-dependent decrease in short-circuit current (SCC) and increase in transepithelial electrical resistance.
  • HY-101453
    Ceefourin 1

    Others Cancer
    Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
  • HY-121721
    Inz-5

    Fungal Infection
    Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance.
  • HY-100589
    Isepamicin sulfate

    Sch 21420 sulfate

    Bacterial Antibiotic Infection
    Isepamicin sulfate (Sch 21420 sulfate) is a broad spectrum aminoglycoside antibiotic. Isepamicin sulfate exhibits considerable antimicrobial activity against Gram-negative non-fermenters in a region with high antimicrobial resistance.
  • HY-N8615
    Peucedanocoumarin II

    Others Others
    Peucedanocoumarin II can induce rice resistance to blast disease.
  • HY-P2657
    Verucopeptin

    HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-101791
    P-gp inhibitor 1

    P-glycoprotein Cancer
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  • HY-17517
    Tiadinil

    Bacterial Infection
    Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; fungicide.
  • HY-100751
    N-563

    Others Others
    N-563 is an analogue of deoxyspergualin with an immunostimulating activity,it promotes resistance to Candida albicans infection in mice.
  • HY-127026S
    Quinaprilat-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance.
  • HY-121969
    DDX3-IN-2

    HIV Infection
    DDX3-IN-2 is an active DEADbox polypeptide 3 (DDX3) inhibitor with an IC50 value of 0.3 μM. DDX3-IN-2 shows a broad spectrum of antiviral activity. DDX3-IN-2 has the potential to overcome HIV resistance.
  • HY-130613
    MAC-545496

    Bacterial Infection
    MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
  • HY-N3021
    D-chiro-Inositol

    Endogenous Metabolite Metabolic Disease
    D-chiro-Inositol is an epimer of myo-inositol found in certain mammalian glycosylphosphatidylinositol protein anchors and inositol phosphoglycans possessing insulin-like bioactivity. D-chiro-Inositol is used clinically for the treatment of polycystic ovary syndrome (PCOS) and diabetes mellitus, which can reduce hyperglycemia and ameliorate insulin resistance.
  • HY-134004
    Pentoxyverine

    Carbetapentane

    Sigma Receptor Neurological Disease
    Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
  • HY-16700
    PNU-159682

    ADC Cytotoxin Topoisomerase Cancer
    PNU-159682, a metabolite of the anthracycline nemorubicin, is a highly potent DNA topoisomerase I inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome drug resistance.
  • HY-125588
    Chromium picolinate

    Chromium (III) picolinate; Cr(Pic)3

    Others Metabolic Disease
    Chromium picolinate (Chromium (III) picolinate) reduces insulin resistance and has the potential for type 2 diabetes mellitus.
  • HY-100390
    (S)-ML753286

    BCRP Cancer
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  • HY-B0826
    Spirodiclofen

    BAJ-2740

    Parasite Infection
    Spirodiclofen is a broad spectrum acaricide acting via lipid biosynthesis inhibition (LBI) with no cross resistance to currently available acaricides and with additional insecticidal properties.
  • HY-12779
    Cyantraniliprole

    HGW-86

    Others Others
    Cyantraniliprole(HGW-86) is an insecticide of the ryanoid class; has activity against pests such as Diaphorina citri that have developed resistance to other classes insecticides.
  • HY-N6004
    (Rac)-Shikonin

    Shikalkin

    Others Cancer
    (Rac)-Shikonin (Shikonin) possesses anti-tumor activity. (Rac)-Shikonin (Shikonin) circumvents cancer drug resistance by induction of a necroptotic death.
  • HY-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • HY-134004S
    Pentoxyverine-d8

    Sigma Receptor Neurological Disease
    Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
  • HY-N9410
    Lysophosphatidylcholine 18:2

    1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC

    Endogenous Metabolite Metabolic Disease
    Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment.
  • HY-N5003
    Columbianetin

    Others Infection Inflammation/Immunology
    Columbianetin is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory activity.
  • HY-107643
    Reversan

    CBLC4H10

    P-glycoprotein Cancer
    Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
  • HY-N4244
    Kakkalide

    Others Inflammation/Immunology
    Kakkalide is an isoflavone derived from the flowers of Pueraria lobata. Kakkalide ameliorates endothelial insulin resistance by suppressing reactive oxygen species (ROS)-associated inflammation.
  • 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-132923
    NBTIs-IN-4

    Bacterial Infection
    NBTIs-IN-4 demonstrates potent antibacterial activity against diverse Gram-positive pathogens, inhibition of both DNA gyrase and topoisomerase IV, a low frequency of resistance.
  • HY-121793
    Roemerine

    (-)-Roemerine

    P-glycoprotein Cancer
    Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
  • HY-17036
    Naphthoquine phosphate

    Parasite Infection
    Naphthoquine phosphate is a potent and orally active antimalarial agent. Naphthoquine phosphate has thorough killing function for various schizonts of plasmodia, including resistance of P. falciparum to Chloroquine.
  • 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-115716
    EGFR-IN-17

    EGFR Cancer
    EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
  • HY-14620
    α-Farnesene

    Others Others
    α-Farnesene is classified as a sesquiterpene, and is a herbivore-induced plant volatile (HIPV). α-Farnesene has an important effect on insect resistance in many plant species.
  • HY-118828
    12-Oxo phytodienoic acid

    12-OPDA

    Bacterial Infection
    12-Oxo phytodienoic acid is a biologically active, immediate precursor of 7-epi jasmonic acid. 12-Oxo phytodienoic acid plays an independent role in mediating resistance to pathogens and pests.
  • HY-N0425
    Epoxylathyrol

    P-glycoprotein Cancer
    Epoxylathyrol, an epoxylathyrane derivative isolated from the Euphorbia boetica, is a P-glycoprotein (P-gp) inhibitor. Epoxylathyrol is a P-gp-mediated multidrug resistance (MDR) reverser.
  • HY-B0384
    Temocapril hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Temocapril hydrochloride is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
  • HY-N0363
    (+)-Columbianetin

    (S)-Columbianetin

    Others Infection Inflammation/Immunology
    (+)-Columbianetin is an isomer of Columbianetin. Columbianetin is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory 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-N2103
    Tenacissoside G

    Others Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-P2036
    FSL-1

    Toll-like Receptor (TLR) Antibiotic Infection
    FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
  • HY-N0363A
    (+)-Columbianetin acetate

    (S)-Columbianetin acetate

    Others Infection Inflammation/Immunology
    (S)-Columbianetin acetate is an isomer of Columbianetin. Columbianetin is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory activity.
  • HY-125648
    Euphorbadienol

    alpha-Euphorbol

    Others Infection
    Euphorbadienol (alpha-Euphorbol), a triterpenic compound, isolated from the latex of Euphorbia resinifera. The derivatives of Euphorbadienol can be used as elicitors of disease resistance, and has antileishmanial and antitrypanosomal activity.
  • HY-111414
    Hsp90-Cdc37-IN-1

    HSP Cancer
    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
  • HY-N6684
    Deoxynivalenol

    Others Metabolic Disease
    Deoxynivalenol, a mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors.
  • HY-B0259
    Indapamide

    Potassium Channel Cardiovascular Disease
    Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy.
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  • HY-N9386
    Tellimagrandin II

    Eugeniin

    Bacterial Antibiotic Infection Inflammation/Immunology
    Tellimagrandin II (Eugeniin), the first intermediate in the 4C1-glucose derived series of ellagitannins, also inhibits antibiotic resistance of drug-resistant Staphylococcus aureus.
  • HY-W015343
    3-Methoxyphenylacetic acid

    m-Methoxyphenylacetic acid

    Others Others
    3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot.
  • HY-141487
    CLP-3094

    Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
  • HY-N1916
    Coniferyl ferulate

    Gutathione S-transferase P-glycoprotein Cancer
    Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST), reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM.
  • HY-N4108
    Hypophyllanthin

    P-glycoprotein Cancer Inflammation/Immunology
    Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
  • HY-116815
    Lalistat 1

    Bacterial Infection Neurological Disease
    Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.
  • HY-12757
    YHO-13177

    BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-N1514
    Ganoderenic acid B

    Others Cancer
    Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
  • HY-W011400
    TLR1

    MyD88 Inflammation/Immunology
    TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses.
  • HY-100713S
    Temocapril-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
  • HY-19753
    KS176

    BCRP Cancer
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
  • HY-111425
    SSE15206

    Microtubule/Tubulin Apoptosis Cancer
    SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin

    Others Metabolic Disease
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
  • HY-135337
    Ethyl tosylcarbamate

    Potassium Channel Metabolic Disease
    Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877). Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
  • HY-108230
    ALK-IN-12

    ALK Cancer
    ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
  • HY-N5124
    Meloside A

    Isovitexin 2''-O-glucoside; Isovitexin 2''-O-β-D-glucoside

    Others Infection
    Meloside A (Isovitexin 2''-O-glucoside) is a phenylpropanoid isolated from barley with antioxidant activity. In barley, phenylpropanoids have been described as having protective properties against excess UV-B radiation and have been linked to resistance to pathogens.
  • HY-N7400
    Phaseoloidin

    Others Others
    Phaseoloidin is a homogentisic acid glucoside from Nicotiana attenuata trichomes and contributes to the plant's resistance against lepidopteran herbivores. Phaseoloidin reduces larval growth of the specialist larvae Manduca sexta and the generalist larvae Spodoptera littoralis. Phaseoloidin has anti-complement activitie.
  • HY-15584A
    Taltobulin trifluoroacetate

    HTI-286 trifluoroacetate; SPA-110 trifluoroacetate

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-136476B
    Cu(II) protoporphyrin IX

    Others Cancer Inflammation/Immunology
    Cu (II) Protoporphyrin IX is used as a negative control for Zn (II) Protoporphyrin (an inihibitor of heme oxygenase). Heme oxygenase has been implicated in tumor cell resistance to chemotherapy, reduction of free radical formation and inflammation, and associated with vascular repair.
  • HY-B0259S
    (rac)-Indapamide-d3

    Potassium Channel Cardiovascular Disease
    (Rac)-Indapamide-d3 is a labelled racemic Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy.
  • HY-15584B
    Taltobulin hydrochloride

    HTI-286 hydrochloride; SPA-110 hydrochloride

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-B1899A
    Taurodeoxycholic acid sodium hydrate

    Sodium taurodeoxycholate monohydrate

    Caspase Apoptosis Metabolic Disease Inflammation/Immunology
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
  • HY-15584
    Taltobulin

    HTI-286; SPA-110

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-122009
    Indican

    Indoxyl-β-D-glucoside

    Others Others
    Indican (Indoxyl-β-D-glucoside), a glycoside of indoxyl, is a precursor of the dyesindigo and indirubin. Indican has a major metabolite, indoxyl sulfate (IS). IS, an uremic toxin, is a substrate/inhibitor of organic anion transporter (OAT) 1, OAT 3 and multidrug resistance-associated protein (MRP) 4.
  • HY-116494
    ML753286

    BCRP Cancer
    ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
  • HY-123159
    AKI603

    Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
  • HY-B0309
    Felodipine

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-120504
    N-Acetyltyramine

    Bacterial Cancer Infection
    N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
  • HY-14833
    Atiratecan

    TP300

    Others Cancer
    Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.
  • HY-B1245
    Salsalate

    Salicylsalicylic acid; Disalicylic acid

    Reactive Oxygen Species Inflammation/Immunology
    Salsalate, a non-acetylated salicylate, is an effective antirheumatic drug that bypasses gastric absorption and also avoids cyclooxygenase inhibition. Salsalate has anti-inflammatory activity and reduces glucose levels, insulin resistance, and cytokine expression. Salsalate can be used in the research of type 2 diabetes.
  • HY-125331
    DRF-1042

    Topoisomerase ADC Cytotoxin Cancer
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
  • HY-19522
    Seladelpar

    MBX-8025

    PPAR Metabolic Disease
    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  • HY-131723
    Pregnenolone 16α-carbonitrile

    Cytochrome P450 Metabolic Disease
    Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
  • HY-123875A
    Ralaniten triacetate

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-114196
    Aclimostat

    ZGN-1061

    Others Metabolic Disease
    Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells.
  • HY-N5011
    5,7-Dimethoxyflavone

    Cytochrome P450 Cancer Inflammation/Immunology
    5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
  • HY-108592
    UCL 2077

    Others Neurological Disease
    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.
  • HY-N3028
    Taccalonolide B

    Microtubule/Tubulin Cancer
    Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.
  • HY-Y0189
    Methyl Salicylate

    Wintergreen oil

    COX Inflammation/Immunology
    Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
  • HY-B1599
    Chloramphenicol palmitate

    Bacterial Infection
    Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
  • HY-B0947S
    Sulfanitran-d4

    Bacterial Infection
    Sulfanitran-d4 is the deuterium labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
  • HY-107322A
    Barnidipine

    Mepirodipine; YM-09730-5(Free base)

    Calcium Channel Cardiovascular Disease
    Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors. Barnidipine (Mepirodipine) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
  • HY-107322
    Barnidipine hydrochloride

    Mepirodipine hydrochloride; YM-09730-5

    Calcium Channel Cardiovascular Disease
    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
  • HY-139848
    WS-898

    P-glycoprotein Cancer
    WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
  • HY-109189
    Rezivertinib

    BPI-7711

    EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-133675
    Mono(5-carboxy-2-ethylpentyl) phthalate

    MECPP

    Drug Metabolite Others
    Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking.
  • HY-120877
    MRT199665

    Salt-inducible Kinase (SIK) AMPK Apoptosis Cancer
    MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
  • HY-111373
    RapaLink-1

    mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
  • HY-133017
    Amcenestrant

    SAR439859

    Estrogen Receptor/ERR Cancer
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer.
  • HY-116686
    Inz-1

    Cytochrome P450 Fungal Infection
    Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans.
  • HY-15772A
    Osimertinib mesylate

    AZD-9291 mesylate; Mereletinib mesylate

    EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-124952
    iKIX1

    Fungal Infection
    iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
  • HY-125834
    GMB-475

    PROTACs Bcr-Abl Apoptosis Cancer
    GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
  • HY-12203
    PFK-158

    Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • HY-15772
    Osimertinib

    AZD-9291; Mereletinib

    EGFR Cancer
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-128350A
    FGTI-2734 mesylate

    Farnesyl Transferase Cancer
    FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • HY-101511
    TTT-28

    P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
  • HY-131334
    AMPK activator 4

    AMPK Metabolic Disease
    AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
  • HY-132670S
    (S)-(-)-Felodipine-d5

    Calcium Channel Autophagy Cardiovascular Disease
    (S)-(-)-Felodipine-d5 is the deuterium labeled (S)-(-)-Felodipine. (S)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-12717AS
    Phentolamine-d4 hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Phentolamine-d4 (Phentolamine-d4) hydrochloride is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    ALK IGF-1R Autophagy Apoptosis Cancer Endocrinology
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
  • HY-136071
    QPX7728 methoxy acetoxy methy ester

    Bacterial Infection
    QPX7728 methoxy acetoxy methy ester is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 43.
  • HY-136070
    QPX7728 bis-acetoxy methyl ester

    Bacterial Infection
    QPX7728 bis-acetoxy methyl ester is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 42.
  • HY-136072
    QPX7728-OH disodium

    Bacterial Infection
    QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
  • HY-128350
    FGTI-2734

    Farnesyl Transferase Cancer
    FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • HY-P2036A
    FSL-1 TFA

    Toll-like Receptor (TLR) MMP HSV Antibiotic Infection
    FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells.
  • HY-141477
    RM-018

    Ras Cancer
    RM-018 is a potent, functionally distinct tricomplex KRAS G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS G12C.
  • HY-N7118
    Clindamycin hydrochloride monohydrate

    Bacterial Antibiotic Infection
    Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla).
  • HY-15772S
    Osimertinib D6

    AZD-9291 D6; Mereletinib D6

    EGFR Cancer
    Osimertinib D6 (AZD-9291 D6) is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-B1455
    Clindamycin

    Bacterial Antibiotic Infection
    Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla).
  • HY-118607
    VU041

    Potassium Channel Parasite Infection
    VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.
  • HY-120801
    APX-115

    Ewha-18278

    NADPH Oxidase Metabolic Disease Inflammation/Immunology
    APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.
  • HY-119198
    NSC745885

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-120801A
    APX-115 free base

    Ewha-18278 free base

    NADPH Oxidase Endocrinology Inflammation/Immunology
    APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base effectively prevents kidney injury.
  • HY-15666A
    Olverembatinib dimesylate

    GZD824 dimesylate; HQP1351 dimesylate

    Bcr-Abl Cancer
    Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity.
  • HY-15666
    Olverembatinib

    GZD824; HQP1351

    Bcr-Abl Cancer
    Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity.
  • HY-N2416
    Taccalonolide A

    Microtubule/Tubulin Apoptosis Cancer
    Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
  • HY-127146
    Platensimycin

    Antibiotic Bacterial
    Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
  • HY-16438
    RRx-001

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • 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-N2118
    Bilobetin

    PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-N4314
    Scutellarein tetramethyl ether

    4',5,6,7-Tetramethoxyflavone

    Bacterial Infection Inflammation/Immunology
    Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial drug resistance via efflux pump inhibition. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation.
  • HY-N7676
    Marein

    AMPK HDAC Metabolic Disease Neurological Disease Cardiovascular Disease
    Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
  • HY-12826
    IMB-XH1

    Bcl-2 Family Bacterial Cancer
    IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1). IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively.
  • HY-117427
    D5D-IN-326

    Others Metabolic Disease
    D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-14913
    Apricitabine

    SPD754; AVX754

    Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
  • HY-14393
    Emodin

    Frangula emodin

    SARS-CoV Casein Kinase Autophagy Cancer
    Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
  • HY-16909
    Leptomycin B

    CI 940; LMB

    CRM1 Fungal Antibiotic Cancer Infection
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  • HY-117391
    AZ-Dyrk1B-33

    DYRK Cancer Metabolic Disease
    AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC50 of 7 nM.
  • HY-N1919
    Ajmalicine

    Raubasine

    Adrenergic Receptor AChE Cardiovascular Disease Endocrinology
    Ajmalicine (Raubasine) is found in herbs of Catharanthus roseus, is an antihypertensive drug used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure. Ajmalicine (Raubasine) is an adrenolytic drug which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. Ajmalicine (Raubasine) acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2.
  • 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.