Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.IC50 value:Target: in vitro: Azimilide blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide blockade of HERG channels expressed in Xenopus oocytes and I(Kr) in mouse AT-1 cells was decreased under conditions of high [K+]e, whereas block of slowly activating I(Ks) channels was not affected by changes in [K+]e [1]. Azimilide suppressed the following currents (Kd in parenthesis): IKr (< 1 microM at -20 mV), IKs (1.8 microM at +30 mV), L-type Ca current (17.8 microM at +10 mV), and Na current (19 microM at -40 mV). Azimilide was a weak blocker of the transient outward and inward rectifier currents (Kd > or = 50 microM at +50 and -140 mV, respectively). Azimilide blocked IKr, IKs, and INa in a use-dependent manner. Furthermore, azimilide reduced a slowly inactivating component of Na current that might be important for maintaining the action potential plateau in canine ventricular myocytes [2]. In guinea pig ventricular myocytes, NE-10064 (0.3-3 microM) significantly prolonged action potential duration (APD) at 1 Hz. At 3 Hz, NE-10064 (0.3-1 microM) increased APD only slightly, and at 10 microM decreased APD and the plateau potential. NE-10064 potently blocked the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 microM), and inhibited IKs (IC50 3 microM) with nearly 10-fold less potency [3].in vivo: NE-10064 (10 mg/kg intravenously, i.v.) reduced (p < 0.05) the incidence (8 of 12) of PES-induced ventricular tachycardia (VT). The cycle length of induced VT was not prolonged by NE-10064 (0.245 +/- 0.046 s predrug vs. 0.301 +/- 0.060 s postdrug). NE-10064 increased ventricular effective refractory period (VERP 166 +/- 5 ms predrug vs. 194 +/- 13 ms postdrug, p = 0.013), prolonged QTc interval (310 +/- 12 ms predrug vs. 350 +/- 16 ms postdrug, p = 0.004) and prolonged the effective refractory period (ERP) of noninfarcted myocardium (p = 0.045) [4].
Sulfacetamide Sodium is an anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections.Target: AntibacterialSulfacetamide is a sulfonamide antibiotic. Sulfacetamide is able to inhibit the growth of all isolated strains. Depending on the type of bacteria concentrations of 0.006 up to 6.4% sodium sulfacetamide proved to be effective. Simultaneously, all patients were treated with sulfacetamide containing ointment and/or eye drops 4 times daily for maximum of 14 days. With swabs taken at intervals of 7 and 14 days no bacterial growth was detected. Sulfacetamide 10% topical lotion, sold under the brand name Klaron or Ovace, is approved for the treatment of acne and seborrheic dermatitis. Sulfacetamide has been investigated for use in the treatment of pityriasis versicolor and rosacea. It may also have anti-inflammatory properties when used to treat blepharitis or conjunctivitis. It is believed to work by limiting the presence of folic acid which bacteria need to survive. It has been suggested that sulfacetamide may also serve as a treatment for mild forms of hidradenitis suppurativa. Sulfacetamide has antibacterial activity and is used to control acne. Some research indicates that sulfacetamide derivatives may act as antifungals by an CYP51A1-independent mechanism [1-4].
CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. IC50 value: 2.7 μM (EC50, for NR2C) and 2.8 μM (EC50, NR2D)Target: NMDA receptorCIQ increases channel opening frequency of recombinant NR2Cor NR2D containing receptors by two-fold (EC50 = 2.7 and 2.8 μM, respectively), with no effect on NR2A or NR2B subtypes. CIQ does not alter the EC50 values for glutamate or glycine on channel opening. CIQ increases channel opening efficiency and enhances NMDA receptor responses. CIQ reduces associated behaviours in schizophrenia models and potentially enhances dopamine release in Parkinson's disease models.
Cephapirin sodium (Cefapirin sodium), a semisynthetic cephalosporin antibiotic, is bactericidal against strains of gram-positive and gram-negative bacteria[1].
Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
MK-0974 is a calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
endo-BCN-PEG2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range[1]. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 µM). Neuroprotective Effect[2].
Fmoc-Abg(N3)-OH is a click chemistry reagent containing an azide group. Fmoc-Abg(N3)-OH has the potential to synthesize peptide nucleic acids (PNA) and peptoids.
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research[1][2].
ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively[1].
STF-31 is an inhibitor of glucose transporter 1 (GLUT1, IC50 = 1 μM).IC50 value: 1 μMTarget: GLUT1in vitro: STF 31 is a glucose uptake inhibitor in RCC (renal cell carcinoma) 4 cells. By limiting glucose uptake in cancer cells, the immense energy requirements for the cancer cell is not met and the cell does not have the resources to rapidly proliferate.STF-31, which selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival. STF-31 decreases glycolysis by decreasing glucose transport and not by inhibiting a particular glycolytic step or enzyme.[1]in vivo: STF-31 selectively targets the von Hippel-Lindau (VHL)-deficient kidney cancer cells. STF-31 inhibits VHL-deficient cancer cells by inhibiting Glut1. Daily intraperitoneal injection of a soluble analogue of STF-31 effectively reduces the growth of tumors of VHL-deficient cancer cells grafted on nude mice. On the other hand, STF-31 appears to be an inhibitor with a narrow cell target spectrum.[2]
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1].
α-Conotoxin GI has high affinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent[1][2][3].
Nonacosadiene is the pheromone of Drosophila melanogaster from a tetrahydrophyridine derivative[1].
Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1)[1].
Polypectate sodium is a major component of cell wall polysaccharides (pectins) and is used as a carbon source and inducer of polygalacturonase. Polypectate sodium can also be used to evaluate alkaline active and alkaline stable pectate lyases from Streptomyces spp. and to study the optimization of polygalacturonase production from Xanthophyllum spp. and reaction conditions[1].
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40[1].
ST-1006 is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 has anti-inflammatory effect[1][2].
Pyroside is a phenolic compound that can be isolated from P. gunnii[1].
Marsdenoside B (compound 8) is a Marsdenoside isolated from Alocasia genus. Marsdenoside B inhibits the growth of tumor cell lines MGC-803 and HT-29 with IC50s of 25.6 μg/mL and 32.4 μg/mL, respectively.
Factor VIIa substrate is a colorimetric substrate for Factor VIIa, that can be measured by absorbance at 405 nm[1].
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease[1].
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis[1].
Novel antitumor agent, inducing PKR-mediated apoptosis and synergizing with IFN
Nα-(2,4-Dinitrophenyl)-L-arginine is an arginine derivative[1].
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis[1].
Macranthoside A is a triterpene glycoside with anti-microbially activity[1].
N-Succinimidyloxycarbonylpropyl methanethiosulfonate is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Microcystin-LR is a potent inhibitor of type 1 and type 2A protein phosphatases (PP1 and PP2A), with IC50s of 1.7 nM and 0.04 nM, respectively. Sequence: Ala-D-Ala-Leu-D-{Bas}-Arg-{Oaa}-D-{Ggu}.