N2-methylguanosine is a modified nucleoside that occurs at several specific locations in many tRNA's.
Efaroxan hydrochloride is a potent and selective α2-adrenoceptor antagonist, antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist and can be used for the research of cardiovascular disease[1][2][3].
MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape[1].
[D-Val22, Phe33] Big Endothelin-1 (16-38), human is a polypeptide.
Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
Chavicol β-D-glucoside is a phenylpropanoid heteroside. Chavicol β-D-glucoside can be isolated from subspecies of Cedronella canariensis[1].
Parishin is a phenolic glucoside isolated from Gastrodia elata. Parishin exhibits antiaging effects and extends the lifespan of yeast via regulation of Sir2/Uth1/TOR signaling pathway[1].
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats[1].
Azido-PEG4-(CH2)3OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM.Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction[1].
(S,R,S)-AHPC-phenol-alkylC6-amine (dihydrochloride) is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC. (S,R,S)-AHPC-phenol-alkylC6-amine incorporates an E3 ligase ligand plus an alkyl linker ready for conjugation to a target protein ligand.
Sodium 2-Methylpropionate-1-13C is the 13C labeled Sodium 2-Methylpropionate[1].
INO-1001 is a potent and selective Poly (ADP-ribose) polymerase (PARP) inhibitor with an IC50 of 0.05-1 μM. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death[1]. INO-1001 has anti-tumor effects[2].
Minretumomab (CC-49) is a mouse anti-TAG-72 (tumor-associated glycoprotein 72) monoclonal antibody and a radioimmunoconjugate. Minretumomab can be used for the research of cancer and radioimmunotherapy (RIT)[1][2].
Bz-RGFFL-4MβNA (Bz-Arg-Gly-Phe-Phe-Leu-4MβNA) is a peptide and can be used fluorogenic substrate[1].
7-Fluorobenzofurazan-4-sulfonic acid ammonium is a fluorescent label. 7-Fluorobenzofurazan-4-sulfonic acid ammonium can be used for detecting dissolved thiol-disulfide (e.g., Cys, GSH)[1].
Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities[1][2].
3-Mercaptopropionic acid-d4 is the deuterium labeled 3-Mercaptopropionic acid[1].
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA[1][2].
(R)-Donepezil is a R-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor[1][2].
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.
CDK12 inhibitor E9 S-isomer (E9, CDK12-IN-E9) is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux; dose-dependently decreases phosphorylated and total RNAPII in THZ1R NB and lung cancer models, competed strongly with bio-THZ1 for binding to CDK12 at low nanomolar ranges, but not CDK7 (>1 uM); exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12; shows more potent antiproliferative activity in THZ1R NB and lung cancer cells with IC50 ranging from 8 to 40 nM than ribociclib, palbociclib, and AZD5438.
Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Sequence: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
Firazorexton is a potent orexin type 2 receptor (OX2R) agonist (patent WO2019027058A1, example 395)[1].
GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist[1].
Quinupristin is a streptogramin antibiotic. Quinupristin blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits[1] [2].
Isochavicine is an alkaloids that can be isolated from Piper retrofractum. Isochavicine inhibits the seedling growth of cress with I50 values of 11 μM[1].
SGC-STK17B-1 is a potent, selective, ATP-competitive inhibitor of death-associated protein kinase family member STK17B (DRAK2) with IC50 of 34 nM, >100-fold selectivity over STK17A;SGC-STK17B-1 is also >100-fold selective over all of the other kinases tested, with only STK17A, CAMKK1, and AURKB (IC50s=5-9 uM) in panel of 403 wild type human kinase assays.SGC-STK17B-1 demonstrated the highest cell potency in the NanoBRET target engagement assay (IC50=190 nM).SGC-STK17B-1 is the first truly potent and selective chemical probe of STK17B.