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side effect

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33

Inhibitors & Agonists

4

Screening Libraries

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100976
    LUF6283

    		Hydroxycarboxylic Acid Receptor (HCAR) Metabolic Disease
    LUF6283 is a potent and orally active HCA(2) partial agonist, with a Ki of 0.55 µM. LUF6283 can achieve the beneficial lipid lowering effect of niacin without producing the unwanted cutaneous flushing side effect .
    LUF6283
  • HY-110080
    Lisuride maleate

    		Dopamine Receptor Neurological Disease
    Lisuride (maleate) is a potent agonist of dopamine with a probably direct action on dopaminergic receptors. Lisuride (maleate) is an ergot derivative. Lisuride (maleate) releases the premenstrual mastalgia without significant side effects .
    Lisuride maleate
  • HY-144036
    DNA-PK-IN-3

    		DNA-PK Cancer
    DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4) .
    DNA-PK-IN-3
  • HY-129748
    SQ-24798

    		Carboxylesterase Others
    SQ-24,798 is a compound that inhibits carboxypeptidase B with high affinity and specificity. Its inhibitory effect may be achieved through the binding of the sulfhydryl group to the zinc ion of the enzyme and specific side chains.
    SQ-24798
  • HY-118499
    Alpiropride

    RIV-2093

    		 Others Endocrinology
    Alpiropride (RIV-2093) is a metoclopramide (HY-17382) analog that is effective in reducing the gastrointestinal side effects of cancer chemotherapy drugs. In animal studies, alpiropride showed a stronger antiemetic effect than metoclopramide .
    Alpiropride
  • HY-14753
    Rosonabant

    		Cannabinoid Receptor Cardiovascular Disease Metabolic Disease
    Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder .
    Rosonabant
  • HY-118242
    RU 45144

    		Estrogen Receptor/ERR Calmodulin Others
    RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
    RU 45144
  • HY-A0140
    Drotaverine

    		Others Neurological Disease
    Drotaverine is a selective phosphodiesterase 4 inhibitor with angina relief activity. Drotaverine is used to suppress angina, including pain in the gastrointestinal tract and biliary tract. Drotaverine may also cause compound-induced priapism, a side effect of sustained penile erection .
    Drotaverine
  • HY-147821
    CB1-IN-2

    		Cannabinoid Receptor Metabolic Disease
    CB1-IN-2 (Compound 4g) is a selective CB1 inhibitor with an IC50 of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .
    CB1-IN-2
  • HY-147195
    QH536

    		HMG-CoA Reductase (HMGCR) Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    QH536 (Compound 29) is a potent HMGCR degrader with an EC50 of 0.22 μM. QH536 has no side-effect of inducing cholesterol accumulation in cells. QH536 shows anti-inflammatory and can be used for cardiovascular disease and nonalcoholic steatohepatitis research .
    QH536
  • HY-119385
    Savoxepin mesylate

    		Dopamine Receptor Neurological Disease
    Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
    Savoxepin mesylate
  • HY-B0557
    Bisacodyl

    		Dopamine Transporter Opioid Receptor Metabolic Disease Cancer
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect .
    Bisacodyl
  • HY-143585
    CDK9-IN-14

    		CDK Cancer
    CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
    CDK9-IN-14
  • HY-W709349
    Flupirtine hydrochloride

    D 9998 hydrochloride

    		 Potassium Channel iGluR Inflammation/Immunology
    Flupirtine hydrochloride (D 9998 hydrochloride) is a selective neuropotassium channel opener with analgesic activity. Flupirtine hydrochloride is used to inhibit a variety of pain conditions, including chronic musculoskeletal pain, migraines, and neuralgia. Flupirtine hydrochloride has antidepressant and antioxidant properties and may increase the analgesic effect in combination therapy with morphine. Flupirtine hydrochloride relieves abnormally increased muscle tension and has a muscle relaxant effect. Flupirtine hydrochloride is clinically superior to other drugs, such as tramadol and pantoxan, plus its side effects are better tolerated. Flupirtine hydrochloride has a significant effect on inhibiting neural hyperexcitability and therefore exhibits inhibitory potential in various pain states .
    Flupirtine hydrochloride
  • HY-130666
    Chlorambucyl-proline

    		Endogenous Metabolite Cardiovascular Disease
    Chlorambucyl-proline is a chloroplatinyl amino acid derivative with inhibitory activity against bovine pulmonary vasoconstrictor enzyme. Chlorambucyl-proline reacts with the convertase in a 1:1 ratio, and the removal of its radiolabel indicates that the compound has an irreversible inhibitory effect on the enzyme activity. Chlorambucyl-proline binds to the aspartic acid or glutamic acid side chain of the enzyme by forming an ester bond, resulting in irreversible inactivation of the enzyme. The inactivation rate constant of chlororambucyl-proline increases in the pH range of 5-8, indicating that its effect on the enzyme activity is affected by the pH environment .
    Chlorambucyl-proline
  • HY-14330
    ABT-724

    		Dopamine Receptor Neurological Disease
    ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
    ABT-724
  • HY-103409
    ABT-724 trihydrochloride

    		Dopamine Receptor Neurological Disease
    ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
    ABT-724 trihydrochloride
  • HY-120721
    Lagunamycin

    		Lipoxygenase Cancer
    Lagunamycin is a 5-lipoxygenase inhibitor isolated from the culture medium of Streptomyces sp. AA0310. Lagunamycin has a significant inhibitory activity against rat 5-lipoxygenase with an IC50 value of 6.08 μM. Lagunamycin can effectively inhibit 5-lipoxygenase without causing lipid peroxidation, indicating that it has an effective inhibitory effect without causing side effects.
    Lagunamycin
  • HY-135741
    NYX-2925

    		iGluR Neurological Disease
    NYX-2925 is an orally active NMDAR modulator. NYX-2925 restores levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the mPFC. NYX-2925 shows no effect on CAMKII, and any addictive or sedative/ataxic side effects. NYX-2925 can be used for research of a variety of NMDA receptor-mediated central nervous system disorders .
    NYX-2925
  • HY-B0557R
    Bisacodyl (Standard)

    		Dopamine Transporter Opioid Receptor Metabolic Disease Cancer
    Bisacodyl (Standard) is the analytical standard of Bisacodyl. This product is intended for research and analytical applications. Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect .
    Bisacodyl (Standard)
  • HY-150580
    CYP3A4-IN-2

    		Cytochrome P450 Inflammation/Immunology Cancer
    CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants .
    CYP3A4-IN-2
  • HY-144056
    EGFR-IN-39

    		EGFR Cancer
    EGFR-IN-39 is a potent inhibitor of EGFR. EGFR-IN-39 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-39 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 2) .
    EGFR-IN-39
  • HY-144055
    EGFR-IN-38

    		EGFR Cancer
    EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4) .
    EGFR-IN-38
  • HY-144054
    EGFR-IN-37

    		EGFR Cancer
    EGFR-IN-37 is a potent inhibitor of EGFR. EGFR-IN-37 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-37 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 7) .
    EGFR-IN-37
  • HY-144052
    EGFR-IN-35

    		EGFR Cancer
    EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11) .
    EGFR-IN-35
  • HY-144051
    EGFR-IN-34

    		EGFR Cancer
    EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12) .
    EGFR-IN-34
  • HY-144050
    EGFR-IN-33

    		EGFR Cancer
    EGFR-IN-33 is a potent inhibitor of EGFR. EGFR-IN-33 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-33 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 13) .
    EGFR-IN-33
  • HY-W328882
    3-(2-Aminopropyl)phenol

    		Others Cardiovascular Disease
    3-(2-Aminopropyl)phenol is a biologically active compound with significant blood pressure-raising activity. 3-(2-Aminopropyl)phenol can effectively improve the symptoms of orthostatic hypotension in patients. 3-(2-Aminopropyl)phenol can significantly increase blood pressure at rest and when standing after oral administration. 3-(2-Aminopropyl)phenol can help reduce pathological orthostatic adjustment disorders. 3-(2-Aminopropyl)phenol has a relatively small effect on heart rate, and no significant side effects have been observed .
    3-(2-Aminopropyl)phenol
  • HY-117649
    RU-39411

    		Estrogen Receptor/ERR Cancer
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
    RU-39411
  • HY-138110
    Toladryl

    4-Methyldiphenhydramine

    		 Endogenous Metabolite iGluR Histamine Receptor Neurological Disease Inflammation/Immunology
    Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .
    Toladryl
  • HY-138110R
    Toladryl (Standard)

    		Endogenous Metabolite iGluR Histamine Receptor Neurological Disease Inflammation/Immunology
    Toladryl (Standard) is the analytical standard of Toladryl. This product is intended for research and analytical applications. Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .
    Toladryl (Standard)
  • HY-167939
    (R)-Bambuterol

    		Others Inflammation/Immunology
    (R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
    (R)-Bambuterol
  • HY-117087
    K103

    		Phosphatase Cancer
    K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
    K103

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