Metabolic enzymes, lipid and glucose metabolism and hormone signaling.
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CAS 42464-96-0
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues[1]. NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle…
CAS 90614-48-5
Diprotin A is a tripeptide inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.1 μg/ml).It inhibits degradation of glucagon-like peptide 1 in culture with insulin-secreting BRIN-BD11 rat pancreatic β-cells when used at a concentration of 25 μM.Diprotin A (5…
CAS 1673556-40-5
SW203668 is a potent, tumor-specific inhibitor of stearoyl CoA desaturase (SCD) with better bioavailability than SW208108.
CAS 13647-35-3
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase (3-β-HSD or delta 5-delta 4-isomerase), an essential enzyme for…
CAS 1316695-35-8
LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases.
CAS 84371-65-3
Mifepristone (RU-486) is a potent steroidal antagonist exhibiting subnanomolar affinity for progesterone receptors (PR IC₅₀ = 0.2 nM) and nanomolar activity against glucocorticoid receptors (GR IC₅₀ = 2.6 nM). This dual-receptor modulator competitively blocks…
CAS 53714-56-0
Leuprolide is an agonist at pituitary GnRH receptors. Target: GnRH receptorLeuprorelin is a gonadotrophin-releasing hormone (GnRH) analogue used to treat a wide range of sex hormone-related disorders including advanced prostatic cancer, endometriosis and…
CAS 1627580-64-6
MOTS-c, a mitochondria-derived peptide (MDP), exerts antinociceptive and anti-inflammatory effects through activating AMPK pathway and inhibiting MAP kinases-c-fos signaling pathway.
CAS 57773-63-4
Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferation
CAS 2212020-52-3
LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.
CAS 616202-92-7
LLorcaserin (APD-356)is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic
CAS 668270-12-0
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
CAS 5352-53-4
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].
Eloralintide (LY 3841136) sodium is an AMYR agonist, which is promising for research of type 2 diabetes and obesity.
CAS 150399-23-8
Pemetrexed disodium is a novel antifolate that inhibits the folatedependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase with Kis of 1.3, 7.2, and 65 nM, respectively.
CAS 39674-97-0
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
CAS 1295353-98-8
A peptidic glucagon like peptide 2 (GLP-2) analogue for treatment of type2 diabetes.
CAS 854107-55-4
Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.
CAS 639863-77-7
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
CAS 59-05-2
Methotrexate(WR19039; CL14377) can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.in vitro: In normal T cells, Methotrexate (MTX) produced a…
CAS 65928-58-7
Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis. Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral…
CAS 22978-25-2
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
CAS 163222-33-1
Ezetimibe (SCH 58235) is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor.
CAS 97-77-8
Disulfiram is a specific inhibitor of?aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.
CAS 1429179-07-6
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and…
CAS 298197-04-3
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of…
CAS 53558-25-1
Pyrinuron is an inhibitor of NAMPT and NMNAT2.Pyrinuron is used as a model compound in studies of urea derivatives and their reactivity.Research has explored the effects of this compound on insulin-producing beta cells, providing insights into diabetes…
CAS 1177148-36-5
ML 086 is a potent, specific inhibitor of phosphatase PHOSPHO1 with IC50 of 139 nM, with no activity against TNAP (IC50>100 uM); a useful chemical tool to examine the functional role of this enzyme in skeletal mineralization and soft tissue ossification…
CAS 1001478-90-5
A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM…
CAS 2304621-31-4
LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).
CAS 361187-13-5
NCGC00161856 is identified as the first small-molecule ligand and inverse agonist of the thyroid-stimulating hormone receptor (TSHR). It inhibits basal cAMP production in HEK-EM 293 cells that stably express TSHRs, with a half-maximal inhibitory concentration…
CAS 80-05-7
Bisphenol A is a starting material for the synthesis of plastics, primarily certain polycarbonates and epoxy resins, as well as some polysulfones and certain niche materials. It exhibits estrogen-mimicking, hormone-like properties.
CAS 57-88-5
For the detailed information of Cholesterol, the solubility of Cholesterol in water, the solubility of Cholesterol in DMSO, the solubility of Cholesterol in PBS buffer, the animal experiment（test） (test) of Cholesterol, the cell expriment (test) of…
CAS 7659-95-2
In Vitro Betanin is a representative constituent of red beetroot betacyanins, could inhibit peroxynitrite (ONOO-), with an IC50 of 19.2 μM. Betanin also has anti-inflammatory, anti-proliferative effects, nephroprotective activity, cardioprotective activity,…
CAS 79902-63-9
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
CAS 4180-23-8
Trans-Anethole ((E)-Anethole), a phenylpropene derivative isolated from Pimpinella, shows estrogenic activity at lower concentrations and cytotoxic at higher concentrations in cancer cell lines. Trans-Anethole ((E)-Anethole) contributes a large component
CAS 1662711-06-9
DX308 is a potent, selective dual CYP26A1/B1 inhibitor and retinoic acid metabolism blocking agent.DX308 does not interact with off‐target nuclear receptors or CYP450s, is not genotoxic, and is stable in skin, despite vigorous hepatic metabolism.Topical DX308…
GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible…
CAS 1662711-07-0
DX314 is a potent, specific CYP26B1 inhibitor with IC50 of 108 nM, >15-fold selectivity over CYP26A1.DX314 potentiates all-trans-RA (atRA) gene expression effects in healthy and diseased reconstructed human epidermis (RHE).DX314 potentiates the effects of…
TH7127 is a SAMHD1 inhibitor with IC50 of 4.9 μM/4.5 μM/4.0 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively.
CAS 1341-23-7
Nicotinamide riboside is a crystal form of Nicotinamide riboside (NR) chloride. Nicotinamide riboside increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic…
CAS 2924984-09-6
ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces…
CAS 105816-04-4
Nateglinide is an insulin secretagog agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM).Nateglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the…
TH6342 is a SAMHD1 inhibitor with IC50 of 9.1 μM/11.0 μM/5.8 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively. TH6342 engages pre-tetrameric SAMHD1 and deter oligomerization and allosteric activation without occupying nucleotide-binding pockets.
CAS 353-09-3
RGX-202 is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of…
CAS 1449240-68-9
K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.IC50 value: 4.3 uM [1]Target: SphK2in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of…
