α-Latrotoxin, a potent neurotoxin from black widow spider venom, triggers synaptic vesicle exocytosis from presynaptic nerve terminals[1].
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects[1]. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones[2].
CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
Hyaluronan synthase is a membrane protein that requires only Mg+2 and two sugar-UDP substrates (GlcUA-UDP and GlcNAc-UDP) to polymerize HA chains. Hyaluronan synthase catalyzes the biosynthesis of hyaluronic acid (HA)[1][2].
Hydroxysaikosaponin C is a natural product that can be isolated from the root of Bupleurum falcatum[1].
ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).IC50 value: 4 nM/16 nM(thallium influx fluorescent assay/automated electrophysiology assay) [1]Target: KCNK3 blockerML365 possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.
6-Methoxynaringenin is a natural flavonoid that inhibits NO production with an IC50 of 25.8 μM[1].
Kaliotoxin (1-37) is a toxin from the scorpion Artdroctonus mauretanicus mauretanicus. Kaliotoxin (1-37) is a potent calcium-dependent potassium channel blocker[1].
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
GsMTx4 is a spider venom peptide that selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[1]. GsMTx4 significantly attenuates bladder hyperactivity[2].
Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
O-Benzyl-D-serine is a serine derivative[1].
Propargyl-PEG4-NHS ester is a nonclaevable 4-unit PEG linker for antibody-drug-conjugation (ADC).
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug[1][2].
Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells[1].
Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
Chavicol β-D-glucoside is a phenylpropanoid heteroside. Chavicol β-D-glucoside can be isolated from subspecies of Cedronella canariensis[1].
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats[1].
INO-1001 is a potent and selective Poly (ADP-ribose) polymerase (PARP) inhibitor with an IC50 of 0.05-1 μM. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death[1]. INO-1001 has anti-tumor effects[2].
3-Mercaptopropionic acid-d4 is the deuterium labeled 3-Mercaptopropionic acid[1].
BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities[1][2].
(R)-Donepezil is a R-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor[1][2].
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA[1][2].
SGC-STK17B-1 is a potent, selective, ATP-competitive inhibitor of death-associated protein kinase family member STK17B (DRAK2) with IC50 of 34 nM, >100-fold selectivity over STK17A;SGC-STK17B-1 is also >100-fold selective over all of the other kinases tested, with only STK17A, CAMKK1, and AURKB (IC50s=5-9 uM) in panel of 403 wild type human kinase assays.SGC-STK17B-1 demonstrated the highest cell potency in the NanoBRET target engagement assay (IC50=190 nM).SGC-STK17B-1 is the first truly potent and selective chemical probe of STK17B.
Mal-VC-PAB-PNP is a cleavable ADC Linker (ADC Linker). Mal-VC-PAB-PNP can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
Astin C (Asterin) is a cyclic pentapeptide with anticancer and anti-inflammatory properties[1].
Cabozantinib is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
3-Cyanovinylcarbazole phosphoramidite is an antiviral drug that inhibits the synthesis of viral DNA. The modified nucleoside in the compound is synthesized by modifying the ribonucleotide with cyano group at the C-3 position, and can be used as a phosphoric acid amide for DNA synthesis[1].