al-1

AL-1 is a GLYCOINOSITOL PHOSPHOLIPID MEMBRANE ANCHOR containing ephrin found in developing tectum. It can mediate the bundling of cortical axons and repel the axonal growth of retinal ganglia axons. It exists in a variety of adult tissues of BRAIN; HEART;

Phos-tag Acrylamide AAL-107 is a polyacrylamide-conjugated phosphate-binding tag that can be used as a tool for visualizing phosphorylated proteins.

CAL-130 is a PI3Kδ and PI3Kγ inhibitor [IC50s: 1.3 and 6.1 nM].

CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM).

CAL-130 Racemate, the racemate of CAL-130, is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.

a-Santal-10-en-12-oic acid is a useful organic compound for research related to life sciences. The catalog number is T124279 and the CAS number is 74642-79-8.

AAL-149, an analog of FTY720 and a TRPM7 inhibitor (IC50 = 1.081 μM), exhibits multiple anti-inflammatory effects without targeting S1P receptors. It is applicable in anti-inflammatory research.

SirReal-1 is an effective and selective inhibitor of Sirt2.

AL-16049 is an FP-Class prostaglandin analog which may be useful in the treatment of glaucoma and ocular hypertension.

CYMAL-1 has a wide range of applications in life science related research.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

Nepafenac (AHR 9434) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of nepafenac is as a Cyclooxygenase Inhibitor. The chemical classification of nepafenac is Nonsteroidal Anti-inflammatory Compounds.

2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4). It activates a nonclassical potassium channel in cerebrovascular smooth muscle and dilates the middle cerebral artery [1]. [1]. Nikhil K Parelkar, et al. 2,2,2-trichloroethanol Activates a Nonclassical Potassium Channel in Cerebrovascular Smooth Muscle and Dilates the Middle Cerebral Artery. J Pharmacol Exp Ther. 2010 Mar;332(3):803-10.

1-Heptadecanol is a long-chain primary alcohol with antibacterial activity derived from Solena amplexicaulis leaves [1]. [1]. Soumendranath Chatterjee, et al. Antibacterial Activity of Long-Chain Primary Alcohols from Solena amplexicaulis Leaves. Proceedings of the Zoological Society volume 71, pages313-319(2018).

2,6-Dichlorodiphenylamine, an analogue of Diclofenac Sodium, exhibits anti-Candida albicans activity. Diclofenac Sodium, a potent and nonselective COX inhibitor, has IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells. [1]. Makoto Urai, et al. Potent Drugs That Attenuate anti-Candida albicans Activity of Fluconazole and Their Possible Mechanisms of Action. J Infect Chemother. 2014 Oct;20(10):612-5.

trans,trans-2,4-Decadienal (trans,trans-2,4-Decadien-1-al) is a product found in Antiaris toxicaria.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Alphitonin is a flavonoid that has been found in L. leptolepis wood.1 It is also a metabolic intermediate that is formed during the catabolism of quercetin by the human gut bacteria E. ramulus.2,3 |1. Chen, K., Ohmura, W., Doi, S., et al. Termite feeding deterrent from Japanese larch wood. Bioresour. Technol. 95(2), 129-134 (2004).|2. Braune, A., Gütschow, M., Engst, W., et al. Degradation of quercetin and luteolin by Eubacterium ramulus. Appl. Environ. Microbiol. 67(12), 5558-55567 (2001).|3. Jaganath, I.B., Mullen, W., Lean, M.E.J., et al. In vitro catabolism of rutin by human fecal bacteria and the antioxidant capacity of its catabolites. Free Radic. Biol. Med. 47(8), 1180-1189 (2009).

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT, is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding [1]. [1]. Naiman, N., et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989; 32(1), 253-256.

3-Hexenal is an unsaturated aldehyde widely used in biochemical experiments and drug synthesis research.

(+)-Fluprostenol (AL-5848), an analogue of prostaglandin F2 alpha, is a prostaglandin F2α receptor PTGFR agonist and decreases the expression of Oviductal glycoprotein 1 (OVGP1).