(S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist[1][2].
Amphotericin B methyl ester hydrochloride is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester hydrochloride is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester hydrochloride disrupts HIV-1 particle production and potently inhibits HIV-1 replication[1][2].
JT001 (NLRP3-IN-19) is a potent, specific and orally active inhibitor of NLRP3. JT001 can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 can be used for the research of nonalcoholic steatohepatitis and liver fibrosis[1].
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].
Digoxin is a potent inhibitor of Na+/K+-ATPase, clinically used to treat arrhythmia and heart failure.
Cyanine 3.5 (Cy3.5 NHS ester) chloride is an analog of Cy3.5 fluorophore. Cyanine 3.5 chloride is a reactive, red fluorescent dye. Cyanine 3.5 chloride is used for labeling of amino-groups in peptides, proteins, and oligonucleotides. (λex=591 nm, λem=604 nm)[1][2].
Ornipressin is a potent vasoconstrictor, hemostatic and renal agent. Sequence: Cys-Tyr-Phe-Gln-Asn-Cys-Pro-{Orn}-Gly-NH2 (Disulfide bridge: Cys1-Cys6).
N-Octyl 4-hydroxybenzoate-d4 is the deuterium labeled N-Octyl 4-hydroxybenzoate[1].
Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) agonist. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation[1].
Aurein 5.2 is an antibiotic antimicrobial peptide[1].
Diprenorphine is a non-selective opioid antagonist with Ki values of 0.017, 0.072 and 0.23 nM against κ-, μ- and δ-opioid receptors, respectively[1]. Diprenorphine can be used for central poststroke pain (CPSP) research[1].
Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.
Fuzapladib (IS-741) is a potent phospholipase A2 inhibitor. Fuzapladib can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibit the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1].
C-12 NBD cholesterol is a cholesterol derivative with a hydrophilic fluorophore tag (NBD: Ex=465 nm, Em=535 nm). C-12 NBD cholesterol can be used to study the utilization and metabolism of cholesterol[1].
2’,3’,5’-Tri-O-benzoyl-5-methoxyuridine 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].
N-(tert-Butoxycarbonyl)-O-(tetrahydro-2H-pyran-2-yl)-L-serine is a serine derivative[1].
Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.IC50 Value: 4 nM [1]Target: microtubulein vitro: Cytotoxic IC(50) values of CA-4 in human bladder cancer cells were below 4 nM. Analyses of cell-cycle distribution showed CA-4 obviously induced G(2)-M phase arrest with sub-G(1) formation. The analyses of apoptosis showed that CA-4 induced caspase-3 activation and decreased BubR1 and Bub3 in cancer cells [1]. The enhanced apoptosis induced by dasatinib plus CA-4 was accompanied by a greater extent of mitochondrial depolarization, caspase-3 activation and PARP cleavage in HO-8910 cells. Furthermore, elevated expression of Mcl-1 led to a reduced apoptosis induced by dasatinib plus CA-4, highlighting that downregulated Mcl-1 was necessary for the potentiating effect of dasatinib to CA-4-triggered apoptosis [2].in vivo: The increased anticancer efficacy of dasatinib combined with CA-4 was further validated in a human HO-8910 ovarian cancer xenograft model in nude mice [2]. There was a significant, concentration dependent increase in mean arterial blood pressure with a maximum increase of about 60% of the baseline MAP at 30 mg/kg of CA4P compared to the saline control. However, there was no significant increase in the cardiac troponin I level after CA4P injection [3].Clinical trial: A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome [4].
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment[1][2].
Azathioprine(Azasan, Imuran; BW 57-322) is a drug that suppresses the immune system and is used in organ transplantation and autoimmune disease. Target: Azathioprine is an immunosuppressive antimetabolite pro-drug. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. Azathioprine is converted into 6-mercaptopurine in the body where it blocks purine metabolism and DNA synthesis. Thus it most strongly affects proliferating cells, such as the T cells and B cells of the immune system. The main adverse effect of azathioprine is bone marrow suppression, which can be life-threatening, especially in people with a genetic deficiency of the enzyme thiopurine S-methyltransferase. It is also listed by the International Agency for Research on Cancer as a Group 1 carcinogen (carcinogenic to humans) [1-3].
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD)[1][2].
Zeylenone, isolated from ethanol extract of the leaves of Uvaria grandiflora Roxb. Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways[1].
UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis[1].
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium[1][2].
Propan-1-amine-dd5 hydrochloride is the deuterium labeled Propan-1-amine hydrochloride[1].
PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
Stylopine hydrochloride (Tetrahydrocoptisine hydrochloride) is an alkaloid compound originally isolated from Corydalis tubers that exhibits anti-inflammatory and anti-parasitic activities[1][2].
DL001, a FKBP12-dependent rapamycin analog, is a selective mechanistic Target Of Rapamycin Complex 1 (mTORC1) inhibitor with an IC50 of 74.9 pM. In cells, DL001 efficiently represses elevated mTORC1 activity and restores normal gene expression to cells lacking a functional tuberous sclerosis complex. DL001 inhibits mTORC1 signaling without impairing glucose homeostasis and with substantially reduced and no side effects on lipid metabolism and the immune system in vivo in C57BL/6J mice[1].
Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis[1].
Disomotide (G209-2M) is a melanoma antigen that enhances the generation of cytotoxic T lymphocytes (CTL) recognizing native G209 as well as melanoma[1][2].
AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects[1].