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high in vitro permeability

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8

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15197

    Acyltransferase Metabolic Disease
    ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1 .
    ABT-046
  • HY-135797A
    DB1976 dihydrochloride
    4 Publications Verification

    Apoptosis Cancer
    DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect .
    DB1976 dihydrochloride
  • HY-138648

    ERK Neurological Disease
    PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
    PB1
  • HY-112624B

    Dextran 70; Dextran D70; Dextran T70(MW 64000-76000)

    Bacterial Others
    Dextran 70,000 is a high molecular weight polysaccharide formed by glucose linked by α-(1→6) glycosidic bonds. Dextran 70,000 can expand blood volume through colloidal osmotic pressure effect and inhibit cell adhesion and platelet aggregation through steric hindrance. At the same time, Dextran 70,000 can be used as a drug carrier to achieve targeted delivery through endocytosis. Dextran 70,000 is biologically inert and has low immunogenicity. It can be used for clinical blood volume expansion, anti-thrombotic research, and evaluation of vascular permeability in in vitro experiments. It can also be combined with fluorescent dyes for cell tracking and drug delivery research. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance.
    Dextran T70 (MW 70,000)
  • HY-144660

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
    AChE-IN-7
  • HY-151247

    GnRH Receptor Cancer
    GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing .
    GnRH-R antagonist 1
  • HY-135797

    Apoptosis Cancer
    DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect .
    DB1976
  • HY-121081

    CDK Cancer
    BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
    BAY-958

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