Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
Biotinyl-NH-PEG3-C3-amido-C3-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(19Z)-Normacusine B, Gelsemiurn alkaloids, is a natural product that can be isolated from Gelsemiurn[1].
Effusol, a phenolic constituent from Juncus effuses, exhibits potent scavenging activity for DPPH and ABTS radicals, with IC50 values of 79 μM and 2.73 μM, respectively. Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline[1].
CCK2R ligand CRL is a ligand-linker conjugate; which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker[1].
SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect[1].
Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
Uridine-5-oxyacetic acid 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].
Bananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 2.3 μM.
Fl-DIBO (fluorogenic dibenzocyclooctyne) is a selective and high sensitivity fluorescent probe to azide compounds. Fl-DIBO can react rapidly with azide compounds to form new highly fluorescent products with a maximum emission wavelength of 469 nm and excitation wavelength of 363 nm. Fl-DIBO can be used to label diazo-tagged proteins without detectable background signal interference[1][2].
Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells[1][2][3].
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo[1].
Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity[1][2].
LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays.
hCAIX/XII-IN-4 (compound 6c) is a potent CAIX/XII inhibitor with the Ki values of 4.5 nM, 23.6 nM, >10000 nM and >10000 nM for CAXII, CAIX, CAI and CAⅡ, respectively[1].
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury[1][2].
Anti-inflammatory agent 57 (Compound 13), pyranocoumarin, is a nature product. Anti-inflammatory agent 57 can be isolated from the roots of Peucedanum praeruptorum. Anti-inflammatory agent 57 has multidrug-resistance (MDR) reversal and anti-inflammatory effect[1].
Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes[1].
4-Hydroxyindole is a member of the class of hydroxyindoles that is 1H-indole substituted by a hydroxy group at position 4. 4-Hydroxyindole is an important raw material or intermediate in the synthesis of pharmaceutical products and industrial polymers[1].
Flavanomarein is a predominant flavonoid of Coreopsis tinctoria Nutt with protective effects against diabetic nephropathy. Flavanomarein has good antioxidative, antidiabetic, antihypertensive and anti-hyperlipidemic activities[1][2].
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2 activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity[1].
3′-Azido-2′,3′-dideoxyuridine (AzdU) is a nucleoside analog of Zidovudine (HY-17413). 3′-Azido-2′,3′-dideoxyuridine is a potent inhibitor of human immunodeficiency virus (HIV) replication in human peripheral blood mononuclear cells (PBMC) with limited toxicity for human bone marrow cells (BMC)[1][2][3].
Kadsuracoccinic acid A is a tetracyclic natural compound that can be isolated from the stems of Kadsura coccinea. Kadsuracoccinic acid A has vitro anti-HIV-1 activitiy with an EC50 value of 68.7 μM[1].
MJN-228 is a selective ligand for the lipid-binding protein nucleobindin 1 (NUCB1) with IC50 of 3.3 uM (blocks AEA-DA probe labeling of NUCB1); shows no affinity for other arachidonoyl probe-protein interactions in HEK293T cell lysate; a probe used to elucidate the role of NUCB1 in lipid metabolic pathways in cells.
Tenacissoside X (Tenacissoside J) is a compound isolated from Marsdenia tenacissima. Marsdenia tenacissima, a traditional Chinese herbal medicine, has long been used for the research of asthma, tracheitis, rheumatism, etc[1][2].
Hydroxy-PP-Me is a potent and specific CBR1 inhibitor with an IC50 of 759 nM. Hydroxy-PP-Me inhibits serum-withdrawal-induced apoptosis. Hydroxy-PP-Me increases As2O3-induced apoptotic cell death compared with As2O3 alone[1][2].
8-Benzyloxyadenosine is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity[1][2].
Onradivir is a significantly better anti-influenza virus agent extracted from patent WO2021047437 A1.