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Chemical Inhibitors

" in MCE Product Catalog:

82

Inhibitors & Agonists

9

Screening Libraries

1

Fluorescent Dye

1

Biochemical Assay Reagents

1

Peptides

1

MCE Kits

6

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-112670
    Exo1

    Others Others
    Exo1 is a chemical inhibitor of the exocytic pathway.
  • HY-100816
    Rbin-1

    Ribozinoindole-1

    Phosphatase Metabolic Disease
    Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
  • HY-B2119
    Sodium tauroglycocholate

    Tauroglycocholic acid sodium salt

    Others Endocrinology
    Sodium tauroglycocholate is an inhibitor of the biliary acid transporting system of the hepatocyte and also a surfactant used as a chemical permeation enhancer.
  • HY-B1434
    7-Aminocephalosporanic acid

    7-ACA

    Bacterial Antibiotic Infection
    7-Aminocephalosporanic acid is the core chemical structure for the synthesis of cephalosporin antibiotics, is a potent β-lactamase inhibitor.
  • HY-112565
    MBX-4132

    Bacterial Infection
    MBX-4132, a member of a chemical class called oxadiazoles that inhibit trans translation by binding to the bacterial ribosome.
  • HY-52101
    CMK

    Ribosomal S6 Kinase (RSK) Cancer
    CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.
  • HY-B1127
    Betamipron

    N-Benzoyl-β-alanine

    Bacterial Antibiotic Others
    Betamipron is a chemical compound which is used together with Panipenem to inhibit Panipenem uptake into the renal tubule and prevent nephrotoxicity.
  • HY-112445
    SGC3027

    Histone Methyltransferase Cancer
    SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.
  • HY-121649
    AQ4

    Topoisomerase Cancer
    AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines.
  • HY-30236
    5-Bromoindole

    Others Cancer
    5-Bromoindole is a chemical intermediate that can be used for the synthesis of GSK-3 inhibitors and anti-cancer agents.
  • HY-136352
    Adenosine 5'-succinate

    Others Others
    Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
  • HY-107635
    TMN355

    Others Cardiovascular Disease
    TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.
  • HY-111029
    ALX-1393

    GlyT Neurological Disease
    ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.
  • HY-B0866
    Ametryn

    Others Metabolic Disease
    Ametryn, a member of the Triazine chemical family, is a herbicide which inhibits photosynthesis and other enzymatic processes. Ametryn is effective against annual broadleaf weeds and grasses.
  • HY-20587
    CRAC intermediate 1

    CRAC Channel Inflammation/Immunology
    CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9.
  • HY-122186
    SGC-GAK-1

    Cyclin G-associated Kinase (GAK) Cancer
    SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.
  • HY-115499
    MPC-0767

    HSP Cancer
    MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability.
  • HY-133651
    2,2-Dibromopropanoic acid

    Fungal Infection
    2,2-Dibromopropanoic acid is a dibromo product based on propionic acid. Propionic acid is a short chain fatty acid and acts as chemical intermediate. Propionic acid is also a mold inhibitor and widely used in food preservative.
  • HY-128522
    ARS-1323-alkyne

    Ras Cancer
    ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
  • HY-132599
    Lademirsen

    SAR339375; RG-012

    MicroRNA Inflammation/Immunology
    Lademirsen (SAR339375; RG-012) is a single stranded, chemically modified oligonucleotide that binds to and inhibits the function of miR-21. Lademirsen has the potential for Alport nephropathy research.
  • HY-W006230
    Anthraflavic acid

    Others Cancer
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
  • HY-124658
    G0507

    Bacterial Infection
    G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria.
  • HY-120145
    MST-312

    Telomerase Inhibitor IX

    Telomerase Cancer
    MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM).
  • HY-111457A
    BAY-678

    Elastase Inflammation/Immunology
    BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-131991
    Benzyl selenocyanate

    DNA Methyltransferase Cancer
    Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM.
  • HY-N6845
    3-Isomangostin

    DNA/RNA Synthesis Cancer
    3-Isomangostin, extracted from Garciniamangostana.L. shell, is a potent MutT homologue 1 (MTH1) inhibitor with an IC50 value of 52 nM. 3-Isomangostin would be an attractive chemical tool for the development of anticancer agents.
  • HY-Y0413
    Biacetyl monoxime

    Diacetyl monoxime; DAM

    Na+/K+ ATPase Myosin Metabolic Disease
    Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca 2+ release.
  • HY-18961
    PD 407824

    Checkpoint Kinase (Chk) Wee1 Cancer Inflammation/Immunology
    PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-151473
    PIKfyve-IN-1

    PIKfyve Cancer Infection
    PIKfyve-IN-1 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) with IC50 value of 6.9 nM. PIKfyve-IN-1 can be used for the research of PIKfyve in virology.
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-151101
    MS159

    PROTACs Cancer
    MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease.
  • HY-116954
    Metribuzin

    DNA/RNA Synthesis Others
    Metribuzin is a low-cost non-selective herbicide that belongs to the chemical class of triazinones. Metribuzin hinders DNA synthesis in treated plants and acts on photosystem II, ultimately inhibiting photosynthesis. Metribuzin provides good control of important annual grass and broad-leaf weeds.
  • HY-117604
    THPP-1

    Phosphodiesterase (PDE) Neurological Disease
    THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
  • HY-N7069
    4-Isopropylbenzyl alcohol

    Others Cancer
    4-Isopropylbenzyl alcohol is a chemical composition of the essential oils from the leaves and flowers of Camellia nitidissima. C. nitidissima possess multiple biological activities including antioxidant activity, anticancer activity, and cytotoxicity as well as inhibiting the formation of advanced glycation end-products.
  • HY-134673A
    UZH1a

    Apoptosis Cancer
    UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1a can be used for epitranscriptomic modulation of cellular processes. UZH1a has antitumor activity. UZH1a also can be used as a chemical probe for studying METTL3.
  • HY-148136
    sEH inhibitor-7

    Epoxide Hydrolase Inflammation/Immunology
    sEH inhibitor-7 (compound c-2) is an inhibitor of soluble epoxide hydrolase (sEH) with IC50s of 0.15 μM (mouse sEH) and 6.2 μM (human sEH), respectively. soluble epoxide hydrolase (sEH) plays an important role in the metabolism of endogenous chemical mediators involved in the regulation of blood pressure and inflammation.
  • HY-D0226
    Quinizarin

    1,4-Dihydroxyanthraquinone

    DNA/RNA Synthesis Fungal Cancer Infection
    Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
  • HY-19313
    LLY-507

    Histone Methyltransferase Cancer
    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
  • HY-132308
    DYRK1-IN-1

    DYRK Neurological Disease
    DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
  • HY-123781A
    RUSKI-201 dihydrochloride

    Hedgehog Cancer
    RUSKI-201 dihydrochloride is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 0.20 μM. RUSKI-201 dihydrochloride is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 dihydrochloride is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function.
  • HY-150064
    SARS-CoV-2 nsp3-IN-2

    Others Infection
    SARS-CoV-2 nsp3-IN-2 is a macrodomain (Mac1) inhibitor with IC50 value of 180 μM. SARS-CoV-2 nsp3-IN-2 is a small molecule chemical probe and can be used for the research of viral.
  • HY-W017132
    2,4-PDCA

    Histone Demethylase Cancer
    2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics.
  • HY-111515
    BAY-678 racemate

    Elastase Inflammation/Immunology
    BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-148242
    BAY-069

    Others Cancer
    BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer.
  • HY-90006
    5-Fluorouracil

    5-FU

    Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-P3581
    PE 22-28

    Potassium Channel Neurological Disease
    PE 22-28 is a TREK-1 inhibitor with IC50 value of 0.12 nM. PE 22-28 also is a 7 amino-acid peptide that is used as a core sequence for preparing analogs by chemical modifications and also by substitution of amino-acids. PE 22-28 can be used for the research of depression.
  • HY-114398
    BAY-293

    Ras Cancer
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-101122
    LX2761

    SGLT Metabolic Disease
    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  • HY-148234
    M4K2234

    Anaplastic lymphoma kinase (ALK) Cancer
    M4K2234 (compound 26b) is an ALK2 inhibitor. M4K2234 inhibits ALK2 and ALK5 with IC50s of 5 and 2144 nM, respectively. M4K2234 can be used as a chemical probe for ALK1 and ALK2 protein kinases. M4K2234 can be used for the research of cancer.
  • HY-111457
    BAY-677

    Others Inflammation/Immunology
    BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-33838
    eIF4A3-IN-8

    Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor 4A3 (eIF4A3) inhibitor. eIF4A3-IN-8 can serve as a valuable chemical probe to elucidate the detailed function of eIF4A3 and EJC (exon junction complex).
  • HY-126154
    L48H37

    Toll-like Receptor (TLR) Inflammation/Immunology
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
  • HY-100201
    A-196

    Histone Methyltransferase Cancer
    A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-N0445
    2-Hydroxy-4-methoxybenzaldehyde

    Tyrosinase Bacterial Others
    2-Hydroxy-4-methoxybenzaldehyde, a chemical compound and an isomer of Vanillin, could be used to synthesis Urolithin M7. 2-hydroxy-4-methoxybenzaldehyde is a potent tyrosinase inhibitor from three East African medicinal plants, Mondia whitei, Rhus vulgaris Meikle, and Sclerocarya caffra Sond.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N1724
    Concanamycin A

    Antibiotic X 4357B; Folimycin; X 4357B

    Proton Pump Bacterial Antibiotic Cancer Infection Inflammation/Immunology
    Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H +-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research -.
  • HY-15221
    Methylstat

    Apoptosis Histone Demethylase MDM-2/p53 Cancer Cardiovascular Disease
    Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.
  • HY-101121
    NI-42

    Epigenetic Reader Domain Cancer
    NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
  • HY-136093
    HL271

    IM156 hydrochloride; HL156A hydrochloride

    AMPK Cancer Neurological Disease
    HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-136093A
    IM156

    HL156A; HL271 acetate

    AMPK Cancer Neurological Disease
    IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-125858
    MI-1061

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-139810
    ETP-47037

    PI3K Others
    ETP-47037 is a potent and inhibitor of PI3Kα isoform with an IC50 value of 0.99 nM. ETP-47037 also inhibits the PI3Kβ, PI3Kδ, and PI3Kγ isoforms, with IC50 values of 49.2, 7.13, and 49.1 nM, respectively. ETP-47037 has the potential for the research of chemical modulation of telomere protection.
  • HY-122630
    TH-257

    LIM Kinase (LIMK) Cancer
    TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
  • HY-134673
    UZH1

    Apoptosis Cancer
    UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3.
  • HY-100338
    CNX-500

    Btk Cancer
    CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
  • HY-151813
    NNMT-IN-4

    Others Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
  • HY-112804
    SGC-iMLLT

    Epigenetic Reader Domain Cancer
    SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.
  • HY-125858A
    MI-1061 TFA

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-90006S2
    5-Fluorouracil-15N2

    Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil-15N2 is the 15N-labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-90006S
    5-Fluorouracil-d1

    5-FU-d1

    Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil-d1 (5-FU-d1) is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-D1640
    5',5-Difluoro BAPTA tetrapotassium

    Others Others
    5,5'-Difluoro BAPTA tetrapotassium is a difluoro-derivative of BAPTA (HY-100168). 5,5'-Difluoro BAPTA tetrapotassium shows large 19F NMR chemical shifts upon chelating divalent cations. 5,5'-Difluoro BAPTA tetrapotassium has high selectivity for Ca 2+. 5,5'-Difluoro BAPTA tetrapotassium can inhibit the growth of pollen tube.
  • HY-12596
    JNJ-26489112

    Calcium Channel Sodium Channel Potassium Channel Neurological Disease
    JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
  • HY-106005
    MMV390048

    Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
  • HY-114204
    GSK8814

    Epigenetic Reader Domain Cancer
    GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.
  • HY-149026
    GNE-064

    Epigenetic Reader Domain Others
    GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.
  • HY-132595
    Teprasiran

    QPI-1002

    MDM-2/p53 Cancer
    Teprasiran (QPI-1002) is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI).
  • HY-112626
    CDK12-IN-2

    CDK Cancer
    CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.
  • 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-19336
    BAZ2-ICR

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
  • HY-135985
    DCLK1-IN-1

    Others Cancer
    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).