hCAIX/XII-IN-2 (compound 6a) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 30.0, 3.6 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate[1]. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].
Poly-L-lysine hydrochloride is a nonspecific attachment factor for cells useful in promoting cell adhesion to solid substrates by enhancing electrostatic interaction between negatively charged ions of the cell membrane and the culture surface. Poly-L-lysine is a strong-attraction regulator that promotes liquid-liquid phase separation (LLPS) at low concentrations but suppresses LLPS at high concentrations. Antibacterial cationic peptide.[1].
Pivalic acid-d9 is the deuterium labeled Pivalic acid[1].
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma[1].
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively[1].
USL311 is a selective CXCR4 antagonist, with anti-tumor activity[1].
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD)[1][2].
Aspoxicillin is a broad-spectrum antimicrobial agent against 68 isolates of Actinobacillus pleuropneumoniae with an MIC90 value of <= 0.05 μg/ml. Aspoxicillin has a long half-life in mouse serum of 55 minutes[1][2].
Z-Tyr(Bzl)-OH is a tyrosine derivative[1].
Tiplimotide (NBI-5788) is an altered peptide ligand (APL) designed from an immunodominant region (83-99) of the neuroantigen myelin basic protein (MBP). Tiplimotide can selectively reduce the production of inflammatory cytokines by pathogenic T-cells. Tiplimotide can be used for the research of multiple sclerosis (MS)[1][2].
Trandolaprilate hydrate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate hydrate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity[1][2].
(S)-2-Amino-2-(2-chlorophenyl)acetic acid is a Glycine (HY-Y0966) derivative[1].
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum[1]. Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitory activity[2].
Methyltetrazine-Amine, a tetrazine compound, is used for the site-specific dual functionalization of the resulting bioconjugates[1].
AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases[1].
SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
1-Methylpyrene is a fluorescent probe and is also a carcinogen in rodents (λex = 346 nm; λem = 378 nm)[1].
Sweroside, isolated from Lonicera japonica, exhibits cytoprotective, anti-osteoporotic, and hepatoprotective effect[1][2].
Propargyl-PEG3-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Onjisaponin Z is a natural product isolated from Radix Polygalae.
DL-Alaninol hydrochloride is an alanine derivative[1].
D-Ribulose-13C-1 is the 13C labeled D-Ribulose[1].
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy[1].
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) is a selective COX-1 inhibitor with an IC50 of 30 µM. Teriflunomide impurity 3 is less active against COX-2 (IC50>100 µM)[1].
YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.
(Rac)-SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor having 1,4-dihydropyrano[2,3-c]pyrazole structure. (Rac)-SHIN2 involves in folate or one-carbon metabolism pathways, prevents viral infection. SHMT1 and SHMT2 are the cytosolic and/or mitochondrial isoforms of serine hydroxymethyltransferase, respectively[1].
Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons[1].
Ingenol 20-palmitate (compound 2) is a diterpene that can be found in Euphorbia lath yris[1].