int-2

INT. 2 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T9795，CAS号为 210193-42-3。

Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂，Ki 为 0.626 nM-9.1 nM。它在多种弥漫性大 B 细胞淋巴瘤模型中抑制 MCL-1 的表达。它有效阻断 MCL-1 的转录调节子 CDK9。

Voruciclib hydrochloride is an orally active and selective inhibitor of CDK (Ki: 0.626 nM-9.1 nM).

HDAC3-IN-T247 (HDAC3 inhibitor T247) 是一种具有选择性和有效性的组蛋白去乙酰化酶 3（HDAC3） 抑制剂，具有抗癌和抗病毒活性。HDAC3-IN-T247 以剂量依赖的方式诱导人结肠癌 HCT116 细胞中 NF-κB 乙酰化。HDAC3-IN-T247 抑制癌细胞增殖。

Obeticholic Acid (6-ECDCA，INT-747 )是一种高亲和力、半合成、胆汁酸衍生的 FXR 激动剂，EC50为 99 nM,且能够上调 IκB-α、KLF-2 和 KLF-4 表达。Obeticholic Acid (6-ECDCA，INT-747 )还显示出其治疗肝脂肪变性、炎症和纤维化的潜力，同时增加胰岛素敏感性。

DNS-8254 is a potent and selective Phosphodiesterase 2 (PDE2) inhibitor for the treatment of Memory Disorders (hPDE2a IC50 = 8 nM, Rat Cl-int = 25.6 uL min mg). DNS-8254 demonstrated significant memory enhancing effects in a rat model of novel object reco

Myceliothermophin E is a polyketide-amino acid hybrid fungal metabolite that has been found inT. thermophilusand has anticancer and antimicrobial activities.1,2It is cytotoxic to DLD-1, Hep3B, HepG2, and HGC-27 cancer cells (IC50s = 0.32, 0.42, 0.26, and 0.08 μg/ml, respectively).1Myceliothermophin E is active against methicillin-resistant, but not -sensitive,S. aureus(MICs = 15.8 and >100 μM, respectively).2 1.Gao, Y.-L., Zhang, M.-L., Wang, X., et al.Isolation and characterization of a new cytotoxic polyketide-amino acid hybrid from Thermothelomyces thermophilus ATCC 42464Nat. Prod. Res.Epub ahead of print(2019) 2.Wang, X., Zhao, L., Liu, C., et al.New tetramic acids comprising of decalin and pyridones from Chaetomium olivaceum SD-80A with antimicrobial activityFront. Microbiol.102958(2020)

Octanoic acid-13C is intended for use as an internal standard for the quantification of octanoic acid by GC- or LC-MS. Octanoic acid is a medium-chain saturated fatty acid. It has been found in Teleme cheeses made from goat, ovine, or bovine milk.1 Octanoic acid is active against the bacteria S. mutans, S. gordonii, F. nucleatum, and P. gingivalis (IC80s = <125, <125, 1,403, and 2,294 μM, respectively).2 Levels of octanoic acid are increased in the plasma of patients with medium-chain acyl-CoA dehydrogenase (MCAD) deficiency, an inborn error of fatty acid metabolism characterized by hypoketotic hypoglycemia, medium-chain dicarboxylic aciduria, and intolerance to fasting.3,4 |1. Mallatou, H., Pappa, E., and Massouras, T. Changes in free fatty acids during ripening of Teleme cheese made with ewes', goats', cows' or a mixture of ewes' and goats' milk. Int. Dairy J. 13(1-3), 211-219 (2003).|2. Hyang, C.B., Alimova, Y., Myers, T.M., et al. Short- and medium-chain fatty acids exhibit antimicrobial activity for oral microorganisms. Arch. Oral Biol. 56(7), 650-654 (2011).|3. Onkenhout, W., Venizelos, V., van der Poel, P.F.H., et al. Identification and quantification of intermediates of unsaturated fatty acid metabolism in plasma of patients with fatty acid oxidation disorders. Clin. Chem. 41(10), 1467-1474 (1995).|4. Rinaldo, P., O'Shea, J.J., Coates, P.M., et al. Medium-chain acyl-CoA dehydrogenase deficiency. Diagnosis by stable-isotope dilution measurement of urinary n-hexanoylglycine and 3-phenylpropionylglycine. N. Engl. J. Med. 319(20), 1308-1313 (1988).

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vitro and in vivo.1 |1. Minami, Y., Yoshida, K., Azuma, R., et al. Structure of a novel macrodiolide antibiotic IKD-8344. Tetrahedron Lett. 33(48), 7373-7376 (1992).|2. Hwang, E.I., Yun, B.S., Yeo, W.H., et al. Compound IKD-8344, a selective growth inhibitor against the mycelial form of Candida albicans, isolated from Streptomyces sp. A6792. J. Microbiol. Biotechnol. 15(4), 909-912 (2005).|3. Loutet, S.A., El-Halfawy, O.M., Jassem, A.N., et al. Identification of synergists that potentiate the action of polymyxin B against Burkholderia cenocepacia. Int. J. Antimicrob. Agents 46(4), 376-380 (2015).

L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitorsBioorg. Med. Chem. Lett.24(1)61-64(2014)

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8(1)e55463(2013)

DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue punch cultures of extraplacental membranes. DCVC effects on GBS-stimulated release of pro-inflammatory cytokines from extraplacental membranes in transwell cultures. [1]. Boldenow E, et al. The trichloroethylene metabolite S-(1,2-dichlorovinyl)-l-cysteine but not trichloroacetate inhibits pathogen-stimulated TNF-α in human extraplacental membranes in vitro. Reprod Toxicol. 2015 Apr;52:1-6. [2]. Lash LH, et al. Multigenerational study of chemically induced cytotoxicity and proliferation in cultures of human proximal tubular cells. Int J Mol Sci. 2014 Nov 18;15(11):21348-65. [3]. Yoo HS, et al. Comparative analysis of the relationship between trichloroethylene metabolism and tissue-specific toxicity among inbred mouse strains: kidney effects. J Toxicol Environ Health A. 2015;78(1):32-49.

Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A Puerto Rico 8 34 (H1N1) and A Aichi 2 68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2]. Methyl brevifolincarboxylate exhibits significant DPPH radical scavenging activity with an IC50 value of 8.9 μM. [1]. Wu QY, et al. Chromatographic fingerprint and the simultaneous determination of five bioactive components of geranium carolinianum L. water extract by high performance liquid chromatography. Int J Mol Sci. 2011;12(12):8740-8749. [2]. Fang SH, et al. Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria. J Ethnopharmacol. 2008;116(2):333-340.

Phenylacetyl-coenzyme A (CoA) is a key intermediate in aerobic catabolism of phenylacetate in bacteria such asPseudomonas, when cultured in minimal media using phenylacetate as the sole carbon source.1It is a precursor in the synthesis of the antibiotic penicillin G found in industrial strains ofP. chrysogenum. Phenylacetyl-CoA also acts as an effector molecule of the TetR family transcriptional repressor PaaR inT. thermophilusand the GntR family transcriptional regulator PaaX inE. coliandPseudomonas, binding to each protein to induce derepression of various genes.2

Sphingomyelins (SMs) are bioactive sphingolipids found in mammalian cell membranes.1SMs make up 2-15% of the total organ phospholipid population but are found at higher concentrations in the brain and myelin sheaths surrounding peripheral nerves. They interact with cholesterol to control its distribution within cellular membranes and maintain cholesterol homeostasis in cells. SMs undergo hydrolysis by sphingomyelinase to form ceramides, which are sphingolipid mediators of intracellular signaling.2This product is a mixture of SMs, with variable fatty acyl chain lengths, isolated from buttermilk. [Matreya, LLC. Catalog No. 1329] 1.Slotte, J.P., and Ramstedt, B.The functional role of sphingomyelin in cell membranesEur. J. Lipid Sci. Technol.109(10)977-981(2007) 2.Shayman, J.A.SphingolipidsKidney Int.58(1)11-26(2000)

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions[1][2]. TLQP-21 TFA is a peptide of 21 amino acids. At a dose of 3 μM TLQP-21 induces up to ~69% of the corresponding contraction promoted by acetylcholine[1][2]. [1]. Elena Bresciani , et al. TLQP-21, A VGF-Derived Peptide Endowed of Endocrine and Extraendocrine Properties: Focus on In Vitro Calcium Signaling. Int J Mol Sci. 2019 Dec 24;21(1):130. [2]. Cheryl Cero, et al. The TLQP-21 Peptide Activates the G-protein-coupled Receptor C3aR1 via a Folding-Upon-Binding Mechanism. ructure. 2014 Dec 2;22(12):1744-1753.

93-O17O is a chalcogen-containing cationic lipidoid.1,2It has been used in the generation of lipid nanoparticles (LPNs). LPNs containing 93-O17O localize to the spleen after intravenous injection into mice.1LPNs containing 93-O17O have been used for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice and for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens.3,2 1.Zhao, X., Chen, J., Qiu, M., et al.Imidazole-based synthetic lipidoids for in vivo mrna delivery into primary T lymphocytesAngew Chem. Int. Ed. Engl.59(45)20083-20089(2020) 2.Chen, J., Qiu, M., Ye, Z., et al.In situ cancer vaccination using lipidoid nanoparticlesSci. Adv.7(19)eabf1244(2021) 3.Li, Y., Yang, T., Yu, Y., et al.Combinatorial library of chalcogen-containing lipidoids for intracellular delivery of genome-editing proteinsBiomaterials178652-662(2018)

Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a concentration of 100 μM.3 Dietary administration of collinin (0.05% w/w) reduces the number of mice with tumors and the number of tumors per mouse in a mouse model of colitis-related carcinogenesis.4 |1. Kim, S., Seo, H., Al Mahmud, H., et al. In vitro activity of collinin isolated from the leaves of Zanthoxylum schinifolium against multidrug- and extensively drug-resistant Mycobacterium tuberculosis. Phytomedicine 46, 104-110 (2018).|2. Nguyen, P.-H., Zhao, B.T., Kim, O., et al. Anti-inflammatory terpenylated coumarins from the leaves of Zanthoxylum schinifolium with α-glucosidase inhibitory activity. J. Nat. Med. 70(2), 276-281 (2016).|3. I.S., C., Lin, Y.C., Tsai, I.L., et al. Coumarins and anti-platelet aggregation constituents from Zanthoxylum schinifolium. Phytochemistry 39(5), 1091-1097 (1995).|4. Kohno, H., Suzuki, R., Curini, M., et al. Dietary administration with prenyloxycoumarins, auraptene and collinin, inhibits colitis-related colon carcinogenesis in mice. Int. J. Cancer 118(12), 2936-2942 (2006).