Boc-NH-C4-Br is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
H-D-Phe(4-Me)-OH is a phenylalanine derivative[1].
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1][2].
Sotrastaurin is a potent pan-PKC inhibitor, with Kis of 0.22 nM, 0.64nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1[1][2].
19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively[1].
DSPE-PEG-PDP is a phospholipid PEG conjugate that can be used in drug delivery applications[1].
2-Amino-6-chloropurine-9-(2’-O-propargyl)riboside 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].
Nα-[(9H-Fluoren-9-ylmethoxy)carbonyl]-Nε-tetradecanoyl-L-lysine is a lysine derivative[1].
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
(R)-2-Amino-2-(thiophen-3-yl)acetic acid is a Glycine (HY-Y0966) derivative[1].
BRD3731 is a potent, selective GSK3β inhibitor with IC50 of 15 nM, 14-fold selectivity for GSK3β over GSK3α (IC50=215 nM); displays excellent selectivity in a penal of 311 kinases, displays reduced potency toward the GSK3β mutant (D133E) with IC50 of 53 nM; induces β-catenin stabilization starting at 20 uM in the HL-60 AML cell line, decreases β-catenin S33/37/T41 phosphorylation and induces β-catenin S675 phosphorylation, resulting in increased β-catenin.
Fmoc-Asp(OtBu)-Thr(psi(Me,Me)pro)-OH is a dipeptide.
HBV-IN-6 is a potent HBV inhibitor with an EC50 of 44 nM (WO2021213445A1, compound 3)[1].
NLS (PKKKRKV) is a peptide derived from the simian virus 40 large tumor antigen (SV40 large T antigen), as a method to enhance nuclear entry in the field of gene transfer research[1][2].
Potent, allosteric GPR55 antagonist
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer[1].
CCPA (2-Chloro-N6-cyclopentyladenosine) 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].
Pradofloxacin, a third-generation fluoroquinolone antibacterial agent[1]
Biotinyl-pTH (1-34) (human) is abiotinylated Teriparatide (HY-P0059).
Paneolilludinic acid is a compound isolated from an endolichenic fungus Cryptomarasmius aucubae. Paneolilludinic acid significantly inhibits nitric oxide (NO) production[1].
PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain[1].
Acridone-4-carboxylic acid (ACA) (Compound 2c) is a heme-interacting acridone derivatives that prevents free heme-mediated protein oxidation and degradation. Acridone-4-carboxylic acid inhibits protein carbonyl formation with an IC50 of 43 μM[1].
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor; also an inhibitor of cytidine deaminase with a Ki of 0.95 μM.
Squalane-d62 is the deuterium labeled Squalane[1]. Squalane, found in certain fish oils (especially shark liver oil), and some vegetable oils, is a saturated derivative of Squalene. Squalane shows anticancer, antioxidant, skin hydrating, and emollient activities[2].
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells[1].
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
a-Helical Corticotropin Releasing Factor (12-41) is a 30 amino acids long, α-helical analogue of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH). a-Helical Corticotropin Releasing Factor (12-41) would suppress the stimulatory effect[1][2].