VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.
Proprotogracillin is a steroidal glycoside isolated from the bulbs of lilium speciosum[1].
ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A[1].
Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity[1].
Capivasertib (AZD5363) is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
5-Iodoresiniferatoxin (I-RTX) is a selective TRPV1 antagonist, with an IC50s of 0.7 and 5.4 nM for rat and human receptors, respectively. 5-Iodoresiniferatoxin induces TRPV1-dependent hypothermia in vivo[1].
Deoxynyboquinone (NSC 165572;DNQ) is a potent inducer of cancer cell death that induces death of cancer cells in culture with IC50 of 16-210 nM, a substrate for NAD(P)H:quinone oxidoreductase (NQO1); it's lethality relies on NQO1-dependent futile redox cycling that consumes oxygen and generates extensive reactive oxygen species (ROS).
SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.IC50 Value: 1.0 uM [1]Target: p38 MAPKin vitro: SB 242235 inhibited intracellular p38 activity, human chondrocytes were treated with different doses of SB 242235 prior to stimulation with IL-1_ for 15 min. MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. SB 242235 dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 uM [1].in vivo: SB-242235 demonstrates generally favourable pharmacokinetic properties in all species examined(including rat, dog and monkey). Systemic plasma clearance was high in rat, but in the non-rodent species SB-242235 demonstrated low to moderate clearance with plasma half-lives > 4h. Oral bioavailability in each preclinical species was high. In rat and monkey, SB-242235 demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses [2].In the skin of SKH-1 hairless mice, SB242235, prior to UVB irradiation, blocked activation of the p38 MAPK cascade, and abolished MAPKAPK-2 kinase activity and phosphorylation of HSP27. Moreover, SB242235 inhibited expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2 [3]. The preclinical pharmacokinetics of SB-242235 have been described previously. The present studies were conducted to describe the in vitro metabolic rates and routes of SB-242235 metabolism, to characterize its in vivo preclinical metabolism, and to use these data to aid in the prediction of the pharmacokinetic behaviour of SB-242235 in man [4].
(S)-ATPO is the (S)-enantiomer of ATPO, which is a competitive antagonist at GluR1-4 (AMPA-preferring) receptors[1].
Clavulanate lithium is a potent β-lactamase inhibitor and acts as an antibiotic[1][2].
Astraganoside, an isoflavane compound, isolated from the roots of Astragalus membranaceus (known as ‘‘Huangqi’’)[1].
Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM[1].
Condurango glycoside E0 is a glycoside that can be isolated from Marsdema cundurango[1].
HTBA(3-Hydroxy-2,4,6-triiodobenzoic acid) for your research needs.Off-white to yellow powder.
Adipic acid-d4-1 is the deuterium labeled Adipic acid[1]. Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism[2].
Echinocandin B (A 30912) is an antifungal antibiotic and is the secondary metabolite produced by Aspergillus nidulans[1].
NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.
Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways[1][2].
Lumogallion is a highly sensitive fluorescent reagent for the detection of aluminum, gallium and other metals. Lumogallion has an excitation wavelength of 490 nm and an emission spectrum in the range of 520 nm to 650 nm, with a peak near 580 nm[1][2].
WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM[1][2]. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice[3].
CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1，with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor，particularly androgen receptor，dependent diseases and conditions，such as prostate cancer[1].
Lucifer yellow is a Flurescent Dye, labelling cells by intracellular injection from microelectrodes. Lucifer yellow can be used for studying cell structure and communications. The excitation wavelength is 850 nm and the emission wavelength is 50 nm[1].
CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity [1].
3-(Trifluoromethyl)phenol-d4 is the deuterium labeled 3-(Trifluoromethyl)phenol[1].
PX20606 trans racemate is a FXR agonist with EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.
SYLQDSVPDSFQD, anchor-modified for high-affinity binding to DR4, is a DR4-restricted MHC class II peptide Tyrosinase[1].
Fmoc-L-photo-methionine is a Methionine (HY-13694) derivative[1].
Halofuginone hydrobromide (RU-19110 hydrobromide) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].