Ganodermacetal is a highly oxidized lanostane triterpene, that can be isolated from G. amboinense. Ganodermacetal shows a marked toxicity to brine shrimp larvae[1].
CID-797718 is a compound with unknown details.
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251, is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm)[1][2].
Leucokinin I is a peptide that stimulates contraction of the anterior midgut and hindgut muscles involved in feeding in Rhodnius prolixus but not absorption in the anterior midgut[1].
Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.
Cycloshizukaol A is a symmetrical cyclic lindenane dimer with C2 symmetry. Cycloshizukaol A can be isolated from the root of Chloranthus serratus[1].
7,8-Dihydro-8-oxo-7-propargyl-3’-deoxy-3’-fluoro guanosine 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].
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.
6-Methoxynaringenin is a natural flavonoid that inhibits NO production with an IC50 of 25.8 μM[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.
Hydroxysaikosaponin C is a natural product that can be isolated from the root of Bupleurum falcatum[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.
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1].
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].
Uredepa is an insect chemosterilant. Uredepa can be used for the research of various biochemical studies[1].
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 is under development for the treatment of stress-related disorders[1].
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].
Cys(NPys)-D{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg}-NH2 is a cell-penetrating polypeptide composed of nine arginines and cysteines, used to carry therapeutic agent into the cell[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.
Fmoc-D-Trp(Boc)-OH is a cleavable ADC linker that used in the synthesis of antibody-drug conjugates (ADCs).
Acamprosate D3 calcium is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems[1][2].
DL-Aspartic acid magnesium salt tetrahydrate is an aspartic acid derivative[1].