SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
2’-β-C-Methyl-5-methoxyuridine is a purine nucleoside analogue. 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].
L-Serine isopropyl ester hydrochloride is a serine derivative[1].
AAPH (2,2'-Azodiisobutyramidine dihydrochloride) has an effect of radical generation. AAPH induces oxidative stress and erythrocyte hemolysis[1].
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects[1][2].
Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.IC50 value: Target: IL-12 production inhibitorAddition of increasing concentration of A1 resulted in a dose dependent decrease of IL-12 p40, with maximal inhibition (62.5%) occurring at a dose of 10 μM. tyrphostin A1 blocks CD40L-induced translocation of NF-κB to the nucleus, and reduces the activation of IL-12 p40 gene. In vivo therapy with A1 leads to decrease in generation of myelin basic protein (MBP) specific encephalitogenic T cells. In addition, treatment of SJL/J mice with A1 results in attenuation of experimental allergic encephalomyelitis (EAE) [1]. Tyrphostin A1 is a much weaker inhibitor of TK than other tyrphostins (IC50>1250 μM for epidermal growth factor receptor (EGFR) kinase), and therefore often used to differentiate TK-mediated effects of tyrphostins from other non-specific effects [2].
11(α)-Hydroxynepasaikosaponin k (compound HOSSc) is a saikosaponin that can be found in B. scorzonerifolium Willd[1].
RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively [1].
Griffonilide is a butenolide, isolated from the roots of Semiaquilegia adoxoides, and often occurs alongside lithospermoside[1][2].
(S)-2-((tert-butoxycarbonyl)amino)-3-(o-tolyl)propanoic acid is a phenylalanine derivative[1].
The compound is an a1/a3 adenosine receptor antagonist, which helps to treat (neurological) inflammatory diseases.
Pyrrolidinedithiocarbamate ammonium is a selective NF-κB inhibitor.
Menthyl acetate (L-Menthyl acetate) is a derivative of L-menthol. Menthyl acetate is effective to enhance 5-aminolevulinic acid (ALA) skin permeation[1].
Fmoc-3-Ala(2-thienyl)-OH is an alanine derivative[1].
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[1][2][3].
Boc-L-Homoserine is a serine derivative[1].
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.
ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A[1].
RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
Proprotogracillin is a steroidal glycoside isolated from the bulbs of lilium speciosum[1].
Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
(S)-2-Amino-3-(4-nitrophenyl)propanoic acid hydrate is a phenylalanine derivative[1].
MeOSuc-AAPV-AFC is a biological active peptide. (A highly specific neutrophil elastase substrate, Abs/Em=380/500 nm.)
N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
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].
Azido-PEG8-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].