Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation[1][2][3][4].
Flocoumafen (WL 108366), a second-generation anticoagulant rodenticide (ARs), belongs to the family of vitamin K antagonist (VKA) molecules[1][2].
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade[1].
DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses[1][2].
SARS-CoV-IN-4 (compound 13) is a potent and specific inhibitor of SARS-CoV nsp14 N7-methyltransferase, with an IC50 of 0.6 μM (SARS-CoV nsp14)[1].
1-Boc-2-methyl-4-oxo-D-proline is a proline derivative[1].
(3β,24R)-3-(Acetyloxy)eupha-7,25-dien-24-ol is an euphane triterpene compound isolated from the barks of Broussonetia papyrifera[1].
Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).IC50 value:Target: vitamin D receptorCalcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) displays calcemic actions. Calcitriol stimulates intestinal and renal Ca2+ absorption and regulates bone Ca2+ turnover. Calcitriol (1,25-Dihydroxyvitamin D3; Rocaltrol )exhibits antitumor activity; Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells.
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research[1][2][3].
N-(2,4-Dinitrophenyl)-L-phenylalanine is an alanine derivative[1].
Griseoluteic acid, a phenazine antibiotic, is originally isolated from S. griseoluteus. Griseoluteic acid is a breakdown product of griseolutein A and B[1].
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.IC50 value:Target:in vitro: Dihydrosanguinarine showed much less cytotoxicity than sanguinarine: at the highest concentration tested (20 microM) and 24h exposure, dihydrosanguinarine decreased viability only to 52% [1]. Dihydrosanguinarine showed the highest antifungal activity against B. cinerea Pers, with 95.16% mycelial growth inhibition at 50 μg/ml [2]. dihydrosanguinarine showed the most potent leishmanicidal activities (IC(50) value: 0.014 microg/ml, respectively) [4].in vivo: Repeated dosing of DHSG for 90 days at up to 500 ppm in the diet (i.e. approximately 58 mg/kg/day) showed no evidence of toxicity in contrast to results published in the literature [3].
Urotensin II-related peptide is a human urotensin II anague. Urotensin II-related peptide has high affinity for the UT receptor[1][2].
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.
Guanabenz (hydrochloride) is an oral α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz (hydrochloride) interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz (hydrochloride) also is used for the research of high blood pressure(equivalent).
N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections[1].
ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
Paraquat dichloride is an orally active, fast-acting, non-selective contact herbicide that is absorbed by leaves through some translocation of xylem. The adsorption of Paraquat dichloride is weakly dependent on PH value[1][2][3][4].
BRD9539 inhibits G9a activity with an IC50 of 6.3 μM, inhibits PRC2 activity with a similar IC50.target: G9a, PRC2;IC50: 6.3 μM ( G9a ), 6.3 uM ( PRC2 ); BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration.
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
N-Boc-PEG10-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
RG7800 a small molecule SMN2 splicing modifier to enter human clinical trials to treat spinal muscular atrophy.
Isoanthricin ((Rac)-Deoxypodophyllotoxin) is the racemate of Deoxypodophyllotoxin. Deoxypodophyllotoxin is a potent antitumor and anti-inflammatory agent[1][2].
Acetyl-(D-Arg2)-GRF (1-29) amide (human) is an antagonist of growth hormone releasing factor (GRF). Acetyl-(D-Arg2)-GRF (1-29) amide (human) inhibits the release of growth hormone (GH) and can be used for endocrine research[1].
Diethoxy-phosphorylethyl-PEG5-ethylphosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers[1][2].
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].
Propargyl-PEG4-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].