Rubicordifolin is a natural product that can be isolated from Rubia cordifolia. Rubicordifolin inhibits the growth of sarcoma ascites in mice. Rubicordifolin has significant cytotoxic activity both in vitro and in vivo[1].
I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1].
6-Chloro-1,3,5-triazine-2,4-diamine-13C3 is the 13C3 labeled 6-Chloro-1,3,5-triazine-2,4-diamine.
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM[1].
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1].
Gly-Gly-AMC is a fluorogenic peptide substrate. Gly-Gly-AMC can be used to assess bacterial protease activity of P. aeruginosa and S. aureus[1][2].
7,2′-Dihydroxy-3′,4′-dimethoxyisoflavan 7-O-β-D-glucoside is a bioactive isoflavonoid isolated from Radix Astragali (Huangqi)[1].
(2S)-2-(Acetylamino)-N,4-dimethylpentanamide-d16 is the deuterium labeled (2S)-2-(Acetylamino)-N,4-dimethylpentanamide[1].
PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells[1][2].
1-Pentadecanoyl-2-oleoyl-sn-glycero-3-phosphoinositol-d7 (ammonium) is deuterium labeled 1-Pentadecanoyl-2-oleoyl-sn-glycero-3-phosphoinositol (ammonium).
ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation[1].
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases[1].
5-O-Benzoyl-1,2-di-O-isopropylidene-alpha-D-xylofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
WIT 002 is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
BIO-32546 (example 12b, S-isomer) is an autotaxin (ATX) modulator, extracted from the patent US20170158687A1[1].
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM[1].
Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
CEF14, EBV Rta Protein (28-37) is the HLA A24-restricted epitope from Epstein-Barr Virus Rta protein (28-37).
MK-0429 is a potent integrin antagonist with IC50s of 12.2 nM (α5β1 integrin) and 2.8 nM (αvβ3 integrin), respectively.
I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).IC50 value: 7.3 (pIC50) [1]Target: BRD9in vitro: I-BRD9 is a selective cell active chemical probe for bromodomain containing protein 9 inhibition. I-BRD9, the first selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM[1].
PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.
Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure[1][2][3].
1,2-Distearoyl-sn-glycerol (DSG; 1,2-Dioctadecanoyl-sn-glycerol) acts as an internal standard for Separation and identification of molecular species of 1,2-diacyl-sn-glycerol (DAG)[1].
L-Alanine, N-[(S)-(4-nitrophenoxy)phenoxyphosphinyl]-, 1-methylethyl ester is an alanine derivative[1].
5-Deoxypulchelloside I is a magnoside glycoside that can be isolated from the aerial parts of the Lamiaceae plant Eremostachys laciniata[1].
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA)[1][2].
Ingenol-5,20-acetonide-3-O-angelate is a natural compound.
DFTamP1 is an antimicrobial peptide against Staphylococcus aureus USA300 activity (MIC is 3.1 μM)[1].