Dimethylamino-PEG2-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors. target: GABAA receptorIC 50: GABAA receptor[1]In vitro: In the presence of U93631 at 5 UM, the peak amplitude decreased as a function of GABA concentration, with the half-maximal inhibitory concentration being approximately 100 nM, which is close to the Kd for the high affinity GABA site(85 nM). It appears that the drug interacts with GABA-bound receptors (at least monoliganded) and accelerates receptor desensitization,rather than acting as an open channel blocker. [1]
(+)-Balanophonin is a phenolic compound that could be isolated from Passiflora edulis. (+)-Balanophonin possesses anti-oxidant, anticholinesterase, anti-inflammatory, anticancer, and antineurodegenerative activities[1].
Seviteronel (VT-464) racemate is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity[1][2].
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model[1].
m-PEG5-2-methylacrylate is a PEG- and Alkyl/ester-based PROTAC linker can be used in the synthesis of PROTACs[1].
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity[1].
AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.IC50 value: 24 nM [3]Target: Ack1Ack1 inhibitor AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase [1].The Ack1 inhibitor AIM-100 not only inhibited Ack1 activity but also was able to suppress AR Tyr(267) phosphorylation and its recruitment to the ATM enhancer. Notably, AIM-100 suppressed Ack1 mediated ATM expression and mitigated the growth of radioresistant CRPC tumors [2]. AIM-100, not only inhibited Ack1 activation but also able to suppress pTyr267-AR phosphorylation, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity [3].
7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine[1]. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist[1][2].
Imoxiterol is a β-adrenergic agonist.
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research[1].
Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
H-DL-Phe(4-Me)-OH is a phenylalanine derivative[1].
Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys.
Lomefloxacin (SC47111A) aspartate is a broad-spectrum quinolone antibacterial agent. Lomefloxacin aspartate can be used for researching respiratory tract infections, genitourinary infections, gastrointestinal infections, ENT infections, etc.[1][2].
Ercalcidiol is a metabolite of vitamin D2, is regarded as an indicator of vitamin D nutritional status.
ACPT-II is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects[1][2][3][4][5].
TAT (47-57) GGG-Cys(Npys) is a cell-penetrating peptide (CPP). TAT (47-57) GGG-Cys(Npys) has the potential for intracellular drug delivery research[1].
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
5-Carboxymethylaminomethyluridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Osteostatin (1-5) amide (human, bovine, dog, horse, mouse, rabbit, rat) (Human PTHrP (107-111) amide) is a C-terminal parathyroid hormone-related protein fragment that can inhibit bone resorption[1][2].
Acacetin 7-O-(6′′-O-α-L-rhamnopyranosyl-β-sophoroside) is a flavonoid glycoside isolated from Valeriana jatamansi Jones[1].
Exalamide is an antifungal agent.
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].
D-4-Hydroxyphenylglycine-d4 (D-(-)-4-Hydroxyphenylglycine-d4) is the deuterium labeled D-4-Hydroxyphenylglycine. D-4-Hydroxyphenylglycine (D-(-)-4-Hydroxyphenylglycine) is one of the most important raw materials used in the production of semisynthetic β-lactam antibiotics, such as Amoxicillin (HY-B0467A) and Cefadroxil (HY-B1190)[1].
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction[1].
Odoratisol A is found in Myristica fragrans[1].