PROTAC AR-V7 degrader-2 is an AR-based PROTAC. PROTAC AR-V7 degrader-2 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. PROTAC AR-V7 degrader-2 induces apoptosis[1].
Fmoc-β-Ala-OH is an alanine derivative[1].
BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1)[1].
Dipsanoside A is a novel tetrairidoid glucoside from Dipsacus asper. Dipsacus asper Wall., a perennial plant widespread in China, has been used in traditional Chinese medicine for hundreds of years as a tonic for refreshment, as a fissiparism promoter of the osseous cells, and as an embryo security agent, etc[1].
Eflapegrastim is a humanized IgG4 monoclonal antibody, is also a granulocyte colony-stimulating factor (G-CSF). Eflapegrastim targets to G-CSF receptor (c-Fms). Eflapegrastim stimulates proliferation and differentiation of neutrophil progenitor cells and maintains stable numbers of mature and functional neutrophils. Eflapegrastim also shortens the duration of neutropenia[1].
Ro 22-3581 (4'-(Imidazol-1-yl) acetophenone) is a selective thromboxane (Tx) synthetase inhibitor[1].
H-Asp(Oet)-OEt.HCl is an aspartic acid derivative[1].
Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR)[1].
Denufosol tetrasodium (INS37217) is a long-acting P2Y2 receptor agonist, which exhibits an EC50 of ~10 μM for P2Y2 receptor activation[1].
Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
Momelotinib-d2 (CYT387-d2) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].
DiSC18(3) is a lipophilic carbocyanine dye for membrane labelling[1].
2-Iodohippuric Acid is a Glycine (HY-Y0966) derivative[1].
HDAC6-IN-26 (compound 23) is a potent inhibitor of HDAC6[1].
Sculponeatin B is a diterpenoid compound from the plant of the genus Rabdosia, Labiatae[1].
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors[1].
Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (Substance P (HY-P0201)). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect[1][2].
1-Bromo-2,3,5-trichlorobenzene-d2 is the deuterium labeled 1-Bromo-2,3,5-trichlorobenzene[1].
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases[1][2].
(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-PEG2-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs[1].
(S,R,S)-AHPC-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology[1].
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola[1][2].
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na+-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na+-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells[1].
Methyl N1-demethoxycarbonylchanofruticosinate is an alkaloid isolated from the leaves of Kopsia flavida Blume of the Apocynaceae family[1].
4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression[1].
Cefpodoxime Proxetil is a first oral and broad spectrum antibiotic that belongs to the third generation of cephalosporin. Cefpodoxime Proxetil binds to penicillin binding proteins (PBPs), which inhibits peptidoglycan synthesis, finally results in interfering bacterial cell wall biosynthesis[1].
Suc-AAPK-pNA is a chromogenic substrate for the determination of serine/threonine kinase activity and enzyme kinetic parameters[1].
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing[1].