Phorbol is a highly toxic diterpene, whose esters have important biological properties.
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin[1].
1-(2,3,5-Tri-O-benzoyl-2-C-methyl-β-D-ribofuranosyl)-2,4(1H,3H)-pyrimidinedione is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
Rimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation[1][2].
2,3-Dihydroxy-4-methoxyacetophenone is a neuroprotective compound from Cynenchum paniculatum. 2,3-Dihydroxy-4-methoxyacetophenone improves cognitive function and may has the potential for the treatment of Alzheimer's disease research[1].
MrgprX2 antagonist-4 is an MrgprX2 antagonist extracted from patent US20210128561A1, compound B-51 E117. MrgprX2 antagonist-4 can be used for the research of inflammatory disorders of the skin[1].
Mal-PEG8-Val-Cit-PAB-MMAE is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
ML303 is a pyrazolopyridine influenza virus nonstructural protein 1 (NS1) antagonist (IC90 = 155 nM), with an EC50 of 0.7 μM for Influenza A virus H1N1[1].
NBT(Nitro BT;p-Nitrotetrazolium blue) is a substrate for dehydrogenases; is used with the alkaline phosphatase substrate 5-Bromo- 4-Chloro-3-Indolyl Phosphate (BCIP) in western blotting and immunohistological staining procedures.
Taxayuntin (Taxayunnansin A; 13-Decinnamoyltaxchinin B) is a taxane diterpenoid isolated from Taxus yunnanensis[1].
Methyl 3-O-methylgallate (M3OMG) possesses antioxidant effect and can protect neuronal cells from oxidative damage[1].
EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer[1].
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].
DFP00173 (DFP-00173) is a potent and selective aquaporin-3 (AQP3) inhibitor, inhibits glycerol permeability inerythrocytes with IC50 of 0.2 uM.
Boc-Lys(2-Cl-Z)-OH is a lysine derivative[1].
LY354740 is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
RMI 10874 is a tilorone analogue. Tilorone is a small-molecule, orally bioavailable antiviral agent. RMI 10874 completely abolishes lung colonization of an H-2 negative (GR9.B9) MCA-induced fibrosarcoma clone.
Fmoc-Asp-OtBu is an aspartic acid derivative[1].
Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
p-Hydroxybenzaldehyde-d5 is the deuterium labeled p-Hydroxybenzaldehyde[1]. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations[2].
Isoverticine, a bioactive isosteroidal alkaloid isolated from bulbus of Fritillaria pallidiflora, displays significant cytotoxicity[1].
(R)-3C4HPG is an NMDA receptor antagonist[1].
Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).
BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC[1].
Depramine (GP 31406) is a tricyclic antidepressant with pharmacologically activity. Depramine inhibits acetylcholinesterase，Mg2+-ATPase，and Na+/K+ ATPase activity[1][2].
(R)-(4′-Hydroxy)-5,7-dihydroxy-4-chromanone, a homoisoflavonoid, has antiangiogenic activity against human retinal microvascular endothelial cells[1].
Cyclopropaneacetamide-Exatecan (Compound 2-A) is an ADC Cytotoxin and an Exatecan analogue. Cyclopropaneacetamide-Exatecan can be used in the synthesis of ADC such as anti-B7H3 antibody-Exatecan analogue conjugate (compound ADC-2)[1].
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1[1][2][3].