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;

AL 1965 has anti-neuropathic effects.

AL 1612 is a bio-active chemical.

Heptanal 1,3-glyceryl acetal is a bioactive chemical.

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl/Prkl family of serine/threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

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.

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).

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).

AL-8810, an 11β-fluoro analog of PGF 2α, acts as a selective antagonist at the PGF 2α receptor (FP receptor) [1].

MG-262 is a reversible proteasome inhibitor with multiple biological activities (MGCD-162, Mills 2004) (Morrison et al., 2005, Li et al., 2006) (Tang et al., 2006, Zhang et al., 2007).

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

Decanal, 2-ethylidene- is a biochemical.

Decanal, 2-methylene- is a biochemical.

β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990). β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3 References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990).

Afatinib impurity 11 is a byproduct of Afatinib, an irreversible EGFR family inhibitor with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M, and HER2, respectively[1].