BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research[1].
Beiwutine (10-Hydroxy mesaconitine) is a diester diterpenoid alkaloid[1].
SARS-CoV-2 nsp14-IN-3 (4975) is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 3.5 μM)[1].
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) [1].
Ginsenoside Re is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
(±)-trans-4-Hydroxy-2-hexenal-5,5,6,6,6-dd5 Dimethyl Acetal is the deuterium labeled (±)-trans-4-Hydroxy-2-hexenal Dimethyl Acetal[1].
Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.
6,8-Di-C-β-D-xylopyranoside (compound 3bb) is a xylopyranoside isolated from Dendrobium huoshanensis[1].
LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
DBCO-PEG5-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM[1][2].
Carmoterol hydrochloride is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors. Carmoterol hydrochloride can be used for the research of asthma and chronic obstructive pulmonary disease (COPD)[1][2].
Allylestrenol, a synthetic sexualsteroid, is used worldwide in case of endangered pregnancies.
Z-PDLDA-NHOH is a potent and specific inhibitor of vertebrate collagenase[1].
DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition.
1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity[1][2].
Boc-Arg(Mts)-OH cyclohexylammonium salt is an arginine derivative[1].
Bromo-C10-OBn is a PROTAC linker that can be used in the synthesis of PROTACs.
Protein Kinase C (661-671) is a fragment peptide of β1 subspecies of protein kinase C (PKC). PKC plays a role in cellular growth control and tumor promotion[1][2].
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2].
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease[1].
CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM; no inhibitory activity against c-Kit (>10 uM); inhibits the proliferation of CML cell lines K562 (GI50=14 nM), KU812 (GI50=25 nM), and MEG-01 (GI50=16 nM); completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model with 50 mg/kg/day dosage treatment.
TOOS, a Trinder's reagent, is a novel highly water-soluble aniline derivative; are widely used in diagnostic tests and biochemical tests.
MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects[1].
Dantrolene-13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM)[1][2].
Serplulimab is humanized monoclonal anti-PD-1 antibody[1].
Boc-Phe(3-Br)-OH is a phenylalanine derivative[1].