KP136 is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.
Delpacibart is a humanized, mouse IgG1κ antibody targeting TFRC. TFRC is the most important membrane protein that regulates intracellular iron transport processes[1].
Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons[1].
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.IC50 value:Target: AMPAR modulatorin vitro: PEPA dose-dependently potentiated AMPA-induced increase of [Ca2+]i. In 90% (72 out of 80) of the cells in which cyclothiazide acts, PEPA potentiated the increased [Ca2+]i induced by AMPA with pronounced cell-to-cell variation in rat hippocampal cultures [1]. PEPA bound to the binding domains of the GluA2 and GluA3 flop isoforms of AMPA receptors [2]. coapplication of AMPA with PEPA protected hippocampal CA1 neurons from brain ischemia-induced death. Coapplication of AMPA with PEPA could prevent downregulated expression of GluR2 subunit caused by ischemia and increase BDNF expression via Lyn-ERK1/2-CREB signaling [4].in vivo: PEPA (3, 10, 30mg/kg body weight) or vehicle was intraperitoneally administered into stressed mice once before the first extinction session. The significant decrease of the freezing response in the extinction sessions was only seen in the 30mg/kg PEPA-administered stressed mice, compared with vehicle-administered stressed mice [3].
3'-Methoxy-3,5,4'-trihydroxyflavone-7-neohesperidoside is a flavonoid that can be isolated from Cleome droserifolia. 3'-Methoxy-3,5,4'-trihydroxyflavone-7-neohesperidoside has moderate hepatoprotective activity[1]..
Cannflavin C (compound 5) can be isolated from Cannabis sativa. Cannflavin C has anti-oxidant activity[1].
H-Phe(2,4-DiCl)-OH is a phenylalanine derivative[1].
Clioquinol(Iodochlorhydroxyquin) is an antifungal drug and antiprotozoal compound that shows effectivity for Alzheimer's disease treatment and induce cancer cell death.
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
Hydroxyethyl cellulose is a non-ionic, water soluble, modified cellulose polymer used as a thickening agent for aqueous cosmetic and personal care formulations.
MRS1845 is a Ca2+ channel blocker with relative specificity for store-operated calcium entry (SOCE) channels[1].
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity[1].
Terpin hydrate is an expectorant, commonly used to loosen mucus in patients presenting with acute or chronic bronchitis, and related conditions.
Anle138b is a novel oligomer modulator.
C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING)[1].
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Target: AromataseApproved: October 2005Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM [1]. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells [2]. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells [3].Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats [4].Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors [5].
Zifaxaban is a novel, potent, selective, direct and oral factor Xa inhibitor with IC50 of 11.1 nM (human FXa), displays > 10,000-fold selectivity than other serine proteases; also deoes not impair platelet aggregation induced by collagen, adenosine diphosphate (ADP) or arachidonic acid; significantly prolongs clotting time, prothrombin time (PT), and activated partial thromboplastin time (APTT) in the plasma of humans, rabbits, and rats, with a relatively weak effect on thrombin time; strongly suppresses thrombus formation with ED50 values of 3.09 mg/kg in venous thrombosis models in rats.
TCO-PEG9-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Fmoc-Lys-OH is a lysine derivative[1].
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity[1][2].
Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis[1][2].
SGC-AAK1-1N is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor, with an IC50 of 1.8 μM[1].
Salicylamide is an inhibitor of microsomal UDP-glucuronosyltransferase. Salicylamide is an analgesic and anti-pyretic agent.
Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
Topoisomerase II inhibitor 14 (compound 2f) is a potent inhibtor of Topoisomerase II, with anticancer activity. Topoisomerase II inhibitor 14 induces apoptosis, and arrests cell cycle at S phase. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO[1].
ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
Schisandrin C is a phytochemical lignan isolated from Schizandra chinensis Baill; shows anticancer-effects in human leukemia U937 cells.IC50 value:Target: in vitro: Schisandrin C inhibited cell growth in a dose-dependent manner, which was associated with the induction of G1 arrest of the cell cycle and apoptosis. Schisandrin C induced G1 arrest was correlated with down-regulation of cyclin D1, cyclin E, cyclin-dependent kinase (Cdk) 4 and E2Fs expression, inhibition of phosphorylation of retinoblastoma protein (pRB), and up-regulation of the Cdk inhibitor p21(WAF1/CIP1). In addition, schisandrin C-induced apoptosis was associated with down-regulation of expression of the anti-apoptotic proteins Bcl-2 and Bcl-xL, proteolytic activation of caspase-3 and -9, and a concomitant degradation of poly(ADP-ribose) polymerase (PARP). Furthermore, schisandrin C-induced apoptosis was significantly inhibited by a caspase-3 specific inhibitor z-DEVD-fmk [1]. Schisandrin C was found to reduce nitric oxide (NO) production from LPS-stimulated Raw 264.7 cells. Pre-treatment of Raw 264.7 cells with gomisin J, gomisin N, or schisandrin C reduced the expression of mRNA and the secretion of pro-inflammatory cytokines [2].
Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
2,3-Dimethoxybenzaldehyde (o-Veratraldehyde) is a benzaldehyde analog, with high antifungal activity (MIC=2.5 mM) 2,3-Dimethoxybenzaldehyde (o-Veratraldehyde) could be used for the synthesis of berberine[1].
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research[1].