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pro-drug

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10127
    Barasertib
    Maximum Cited Publications
    25 Publications Verification

    AZD1152

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
    Barasertib
  • HY-124584
    Minnelide
    2 Publications Verification

    Apoptosis Cancer
    Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis .
    Minnelide
  • HY-B0382
    Fosinopril sodium
    3 Publications Verification

    SQ28555

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
    Fosinopril sodium
  • HY-123193

    pro-diazepam

    Drug Intermediate Neurological Disease
    Avizafone (Pro-diazepam), a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone can be used as an antidote of nerve agent poisoning. In vivo, Avizafone is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone has research areas including neurological disease, such as epilepsy .
    Avizafone
  • HY-142209

    Bcl-2 Family Cancer
    ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax .
    ABBV-167
  • HY-153260

    CDK Cancer
    TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor .
    TP-1287
  • HY-Y0267
    Phenoxyacetic acid
    1 Publications Verification

    Insecticide Fungal Phytohormone Infection
    Phenoxyacetic acid is a multifunctional drug prodrug or auxin-type growth regulator, and its derivatives have insecticidal, herbicidal and antifungal activities .
    Phenoxyacetic acid
  • HY-107345

    Ombolan

    Prostaglandin Receptor Inflammation/Immunology
    Droxicam (Ombolan) is a non-steroidal anti-inflammatory agent, with strong analgesic activity. Droxicam acts by inhibiting PGE2 varies, and is characterised by being a pro-drug of Piroxicam (HY-B0253). Droxicam is well tolerated with slight side effects in the said mucosa. Droxicam does not show cardiovascular or respiratory effects in cats, and inhibits peritoneal capillary permeability in mouse .
    Droxicam
  • HY-112068

    HIF/HIF Prolyl-Hydroxylase Cancer
    DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF) .
    DM-NOFD
  • HY-169131

    AMPK Cancer
    ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
    ALKBH1-IN-3 prodrug
  • HY-100085

    21-desDFZ

    Drug Metabolite Inflammation/Immunology
    21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
    21-Desacetyldeflazacort
  • HY-162448

    Drug Intermediate Inflammation/Immunology
    SerBut is a serine conjugated butyrate prodrug with oral activity. SerBut has anti-inflammatory activity .
    SerBut
  • HY-164927

    Influenza Virus Infection Inflammation/Immunology
    AV5124, a prodrug of AV5116, is an orally active influenza virus cap-dependent endonuclease (CEN) endonuclease inhibitor .
    AV5124
  • HY-177716

    Beta-lactamase Bacterial Infection
    Ciprofloxacin prodrug-1 (Compound 35) is an activated prodrug of β-lactase. Ciprofloxacin prodrug-1 exhibits good antibacterial activity against bacteria containing β-lactase (MIC = 63 nM). After being hydrolyzed by β-lactase, Ciprofloxacin prodrug-1 can release Ciprofloxacin (HY-B0356), thereby inhibiting the activity of DNA gyrase. Ciprofloxacin prodrug-1 can be used to study infections caused by enzyme-producing drug-resistant bacteria (such as uropathogenic Escherichia coli) .
    Ciprofloxacin prodrug-1
  • HY-10127A

    AZD1152 dihydrochloride

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152 dihydrochloride), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152 dihydrochloride) induces growth arrest and apoptosis in cancer cells .
    Barasertib dihydrochloride
  • HY-123193S

    pro-diazepam-d5 dihydrobromide

    Isotope-Labeled Compounds Drug Intermediate Neurological Disease
    Avizafone-d5 dihydrobromide is the deuterium labeled Avizafone dihydrobromide . Avizafone (Pro-diazepam) dihydrobromide, a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone dihydrobromide can be used as an antidote of nerve agent poisoning. In vivo, Avizafone is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone dihydrobromide has research areas including neurological disease, such as epilepsy.
    Avizafone-d5 dihydrobromide
  • HY-168635

    PROTACs Epigenetic Reader Domain Cancer
    SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)) .
    SJ46420
  • HY-B1079

    Drug Intermediate Inflammation/Immunology
    Suxibuzone is a compound used for the study of joint and muscle pain, and it is a prodrug of the non-steroidal anti-inflammatory drug Phenylbutazone.
    Suxibuzone
  • HY-126719

    Drug Derivative Neurological Disease
    R-1 Methanandamide Phosphate is a water-soluble prodrug analog of arachidonylethanolamide (AEA). AEA is an endogenous cannabinoid compound .
    R-1 Methanandamide Phosphate
  • HY-175863

    Others Neurological Disease
    2-PMPA prodrug 1 (compound 18b) is an orally active 2-PMPA prodrug with good oral bioavailability .
    2-PMPA prodrug 1
  • HY-168875

    TrxR Reactive Oxygen Species (ROS) Cancer
    TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids .
    TrxR1 prodrug-1
  • HY-179392

    Apoptosis DNA Alkylator/Crosslinker VEGFR PDGFR Cancer
    Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma .
    Sunitinib-platinum(IV) prodrug-1
  • HY-W702001

    pro-diazepam dihydrobromide

    Drug Intermediate Neurological Disease
    Avizafone (Pro-diazepam) dihydrobromide, a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone dihydrobromide can be used as an antidote of nerve agent poisoning. In vivo, Avizafone dihydrobromide is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone dihydrobromide has research areas including neurological disease, such as epilepsy .
    Avizafone dihydrobromide
  • HY-W424539

    Glucocorticoid Receptor Inflammation/Immunology
    Prednisolone (sodium succinate) is an anti-inflammatory corticosteroid and a prodrug of the glucocorticoid prednisolone. Prednisolone (sodium succinate) is used as an immunosuppressant .
    Prednisolone sodium succinate
  • HY-133844

    Drug Intermediate Others
    Bisbentiamine is a lipophilic thiamine prodrug with pH-dependent solubility. The bioavailability of Bisbentiamine is regulated by diet type, administration time, gastric acidity, and formulation .
    Bisbentiamine
  • HY-176810

    STING Cancer
    CDN prodrug-1 (Compound 2) is a STING ligand. CDN prodrug-1 consists of a cyclic dinucleotide (CDN) and a dialanine peptide linker. CDN prodrug-1 can be cleaved following internalization into endolysosomes by cathepsins and subsequently release the parent CDN. CDN prodrug-1 can be used for synthesis nanoparticles for drug delivery research .
    CDN prodrug-1
  • HY-176771

    Drug Intermediate Inflammation/Immunology
    Tapinarof prodrug-1 (Compound 31) is an orally active prodrug of Tapinarof (HY-109044). Tapinarof is an AhR agonist. Tapinarof prodrug-1 has an improving effect in the TNBS-induced mouse model of inflammatory bowel disease. Tapinarof prodrug-1 can be used in the research of inflammatory diseases .
    Tapinarof prodrug-1
  • HY-163849

    Interleukin Related Inflammation/Immunology
    Mizoribine prodrug-1 (compound 18) is a oral active ester-based mizoribine (HY-17470) prodrug. Mizoribine prodrug-1 displays a inhibition of IL-2 production .
    Mizoribine prodrug-1
  • HY-175257

    PARP Reactive Oxygen Species (ROS) Apoptosis NF-κB ERK Bcl-2 Family TGF-β Receptor EGFR Cadherin Cancer
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer .
    Theophylline-platinum(IV) prodrug-1
  • HY-161687

    Src Cancer
    Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
    Cisplatin/Dasatinib prodrug-1
  • HY-174846

    Cannabinoid Receptor TRP Channel Drug Intermediate Neurological Disease Inflammation/Immunology
    TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB2R agonist (EC50: 51.2 nM) and a weak TRPM8 antagonist. TRPM8 antagonist 4 prodrug is a prodrug of TRPM8 antagonist 4 (HY-174825). TRPM8 antagonist 4 prodrug exhibits anti-inflammatory and analgesic activities and can be used in the research of inflammation-related pain disorders .
    TRPM8 antagonist 4 prodrug
  • HY-114249

    Nucleoside Antimetabolite/Analog Dihydropyrimidine Dehydrogenase (DPD) Cancer
    DFP-11207 is an orally active fluoropyrimidine cytotoxic agent. DFP-11207 combines a 5-FU (HY-90006) pro-drug with a reversible DPD inhibitor and a potent inhibitor of OPRT, resulting in enhanced pharmacological activity of 5-FU with decreased gastrointestinal and myelosuppressive toxicities. DFP-11207 can be used for the research of cancer .
    DFP-11207
  • HY-121398

    Adrenergic Receptor Endogenous Metabolite Others
    Dipivefrin is a potent adrenergic agonist. Dipivefrin is an adrenergic pro-agent. Dipivefrin can be used for reduce IOP (intraocular pressure) in patients suffering from chronic open angle glaucoma .
    Dipivefrin
  • HY-Z4483

    Drug Intermediate Others
    6-Deoxypenciclovir is an inactive metabolite of the antiviral prodrug Famciclovir. 6-Deoxypenciclovir is a good substrate for rabbit hepatic aldehyde oxidase and can be used to synthesize the prodrug form of penciclovir .
    6-Deoxypenciclovir
  • HY-119011

    Antibiotic Bacterial Infection
    Pivampicillin is a penicillin antibiotic. Pivampicillin is a prodrug of Ampicillin (HY-B0522) .
    Pivampicillin
  • HY-12758A

    BCRP Cancer
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
    YHO-13351 free base
  • HY-137362

    Drug Intermediate Infection
    N2-Acetyl acyclovir is an Acyclovir prodrug. Acyclovir (Aciclovir) is a potent, orally active antiviral agent .
    N2-Acetyl acyclovir
  • HY-W099488

    Drug Intermediate Cancer
    Capecitabine 2',3'-diacetate (Compound 10b) is the prodrug for the antitumor agent Capecitabine (HY-B0016) .
    Capecitabine 2',3'-diacetate
  • HY-105373

    Drug Intermediate Infection
    PNU 101850 is an Eperezolid (HY-10393) ester prodrug. PNU 101850 acquires antibacterial activity after conversion to the parent drug Eperezolid .
    PNU 101850
  • HY-16622

    LPL Receptor Cardiovascular Disease
    GSK1842799 is an orally active selective S1P1 receptor agonist prodrug. GSK1842799 is promising for research of multiple sclerosis .
    GSK1842799
  • HY-117630

    Drug Intermediate Cancer
    RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice .
    RB-6145
  • HY-163850

    Interleukin Related Inflammation/Immunology
    Mizoribine prodrug-2 trifluoroacetate (compound 20) is a oral active mizoribine (HY-17470) prodrug (amino acid conjugate). Mizoribine prodrug-2 displays a prolonged inhibition of IL-2 production .
    Mizoribine prodrug-2 trifluoroacetate
  • HY-168928

    Bacterial Infection
    Antibiofilm agent prodrug 1 (Compound 5c) exhibits antibacterial activity through inhibition of biofilm formation and iron uptake. Antibiofilm agent prodrug 1 inhibits P. aeruginosa PAO1 with a MIC of 1.07 μM. Antibiofilm agent prodrug 1 exhibits anti-infectious efficacy in C. elegans with improved survival rate .
    Antibiofilm agent prodrug 1
  • HY-161336

    Bacterial Cancer
    Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
    Alendronate prodrug-1
  • HY-172813

    Bacterial Antibiotic Autophagy Infection Cancer
    Vancomycin prodrug (compound 13c) is a Vancomycin (HY-B0671) prodrug. Vancomycin prodrug shows antibacterial effect with MICs of 0.78 μM, 0.78 μM, 1.56 μM for S. aureus 330041, MRSA USA 300 and MRSA 3390, respectively. Vancomycin prodrug has the ability to quickly bind to Cys-34 residue of plasma. Vancomycin prodrug exhibits a good therapeutic effect on MRSA USA300 infected mice similar to Vancomycin. Vancomycin prodrug, an albumin-binding acid-sensitive prodrug, effectively reduces Vancomycin’s nephrotoxicity while maintaining its efficacy for Gram-positive bacterial infections .
    Vancomycin prodrug
  • HY-172148

    Interleukin Related Inflammation/Immunology
    Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid (HY-Y0520) that efficiently delivers the active ingredient Itaconic acid to skin tissue following oral administration. Itaconic acid prodrug-1 possesses immunomodulatory properties, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 can be utilized for the research of alopecia areata and other inflammatory skin diseases .
    Itaconic acid prodrug-1
  • HY-163544

    Drug Intermediate Cancer
    δ-Tocotrienol prodrug-1 (compound 5b) is a prodrug of δ-tocotrienol (HY-122778). δ-Tocotrienol prodrug-1 shows radioprotective efficacy. δ-Tocotrienol prodrug-1 promotes the hematopoietic progenitor and stem cell regeneration in murine bone marrow and spleen .
    δ-Tocotrienol prodrug-1
  • HY-168472

    SARS-CoV Infection
    13-TP prodrug (compound 15) is a potent and orally active anti-SARS-CoV-2 agent. 13-TP prodrug shows cytotoxicity. 13-TP prodrug decreases the SARS-CoV-2 N protein expression. 13-TP prodrug shows antiviral activity .
    13-TP prodrug
  • HY-173023

    Apoptosis Indoleamine 2,3-Dioxygenase (IDO) Reactive Oxygen Species (ROS) Cancer
    IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug. IDOi-Pt(IV) prodrug-1 inhibits IDO expression. IDOi-Pt(IV) prodrug-1 induces apoptosis, decreases the mitochondrial membrane potential, inhibits tumor cell migration and invasion. IDOi-Pt(IV) prodrug-1 induces reactive oxygen species-mediated endoplasmic reticulum stress and secretion of damage-associated molecular patterns (DAMPs), thereby presenting immunogenic cell death (ICD) effects. IDOi-Pt(IV) prodrug-1 has high-efficiency and low-toxicity antitumor effects compared to Cisplatin (HY-17394) .
    IDOi-Pt(IV) prodrug-1
  • HY-176149

    CaMK MMP AMPK Apoptosis Autophagy Cancer
    Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
    Fluoxetine-Conjugated Platinum(IV) prodrug-1

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