k 19

PI3Kα-IN-19 (Compound 1) 为一种定位于p110α催化亚基的PI3Kα抑制剂。作为常见的失调激酶，PI3Kα广泛应用于癌症研究领域。

PI3K-IN-19 hydrochloride (WO2017153220, step 5) acts as a phosphatidylinositol-3-kinase (PI3K) inhibitor.

Vonoprazan fumarate (TAK-438) 是一种新型 P-CAB（钾竞争性酸阻滞剂），可可逆地抑制 H+ K+、ATP 酶。

Vonoprazan Fumarate (TAK438) 是质子泵的有效抑制剂，是口服有效的高效钾竞争性酸阻断剂，具有抗分泌活性。在 pH 为 6.5 时，它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性，IC50为 19 nM。它被开发用于研究酸相关疾病，如消化性溃疡和胃食管反流病。

Proteinase K (Protease K) 是一种非特异性丝氨酸蛋白酶，可以耐受 SDS、尿素、pH 值 (4-12)、盐浓度和温度变化。Proteinase K 可水解多种肽键，用于蛋白消化。

AZ10606120 dihydrochloride 是一种可选择的、有效的、高亲和力的受体拮抗剂，在人和大鼠 P2X 7 受体上的 K D 值分别为 1.4 和 19 nM。AZ10606120 dihydrochloride 抑制肿瘤生长，具有抗血管生成活性 。AZ 10606120在与 ATP 结合位点偶联的位点结合时充当负变构调节剂。

Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg kg. Nitisinone (3 mg kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH- -mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

IT-143B is a bacterial metabolite that has been found in S. iakyrus.1 It inhibits the proliferation of OS-RC-2 and ACHN cancer cells (IC50s = 22 and 98 μM, respectively). |1. Li, K., Liang, Z., Chen, W., et al. Iakyricidins A-D, antiproliferative piericidin analogues bearing a carbonyl group or cyclic skeleton from Streptomyces iakyrus SCSIO NS104. J. Org. Chem. 84(19), 12626-12631 (2019).

6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2.Lee, K., Choi, Y., Gullen, E., et al.Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2',3'-unsaturated L-nucleosidesJ. Med. Chem.42(7)1320-1328(1999)

Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007)

1-thio-β-D-Glucose tetraacetate is a building block.1,2It has been used in the synthesis of aromatic glucosinolates with anti-inflammatory activity, as well as glucosylated poly(pentafluorostyrene) derivatives for coating magnetic iron oxide nanoparticles. 1.Vo, Q.V., Trenerry, C., Rochfort, S., et al.Synthesis and anti-inflammatory activity of aromatic glucosinolatesBioorg. Med. Chem.21(19)5945-5954(2013) 2.Babiuch, K., Wyrwa, R., Wagner, K., et al.Functionalized, biocompatible coating for superparamagnetic nanoparticles by controlled polymerization of a thioglycosidic monomerBiomacromolecules12(3)681-691(2011)

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg/animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

Vonoprazan-d4 是 Vonoprazan 的氘代化合物。Vonoprazan 的 CAS 号为 881681-00-1。Vonoprazan 是一种质子泵抑制剂，是口服活性钾竞争性酸阻断剂，有抗分泌作用。在 pH 为 6.5 时，它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性，IC50值为 19 nM。它可用于研究胃酸相关疾病。

YH-53 是一种有效的3CLpro 抑制剂，对 SARS-CoV-1 3CLpro 和 SARS-CoV-2 3CLpro 的Ki 值分别为 6.3 nM、34.7 nM。YH-53 能够有效阻断 SARS-CoV-2 复制。YH-53 是一种具有独特苯并噻唑基酮的拟肽化合物。YH-53 具有用于研究新冠病毒的潜力。

Ripasudil free base (K-115 (free base)) 是一种ROCK 特异性抑制剂，能够抑制ROCK1和ROCK2的活性，IC50值分别为 51 和 19 nM。

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

GNE-2256 (molecule 19) 是一种具有口服活性的IRAK4(白介素 1 受体关联激酶 4) 抑制剂 (IRAK4Ki=1.4 nM ; IL-6IC50=190 nM)。

Vonoprazan-d3 是 Vonoprazan 的氘代化合物。Vonoprazan 的 CAS 号为 881681-00-1。Vonoprazan 是一种质子泵抑制剂，是口服活性钾竞争性酸阻断剂，有抗分泌作用。在 pH 为 6.5 时，它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性，IC50值为 19 nM。它可用于研究胃酸相关疾病。

6-Hydroxypyridin-3-ylboronic acid is a heterocyclic building block.1,2It has been used in the synthesis of non-nucleoside inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase nonstructural protein 5B (NS5B).16-Hydroxypyridin-3-ylboronic acid has also been used in the synthesis of mammalian target of rapamycin (mTOR) inhibitors.2 1.Hendricks, R.T., Spencer, S.R., Blake, J.F., et al.3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymeraseBioorg. Med. Chem. Lett.19(2)410-414(2009) 2.Verheijen, J.C., Richard, D.J., Curran, K., et al.Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and sselective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituentJ. Med. Chem.52(24)8010-8024(2009)

Vonoprazan hydrochloride 是一种高效且具口服活性的质子泵抑制剂 (PPI) 和钾竞争性酸阻断剂 (potassium-competitive acid blocker, P-CAB)，展示出优秀的抗分泌活性。在 pH 为 6.5 的条件下，该化合物可抑制猪胃微粒体内 H+,K+-ATPase 的酶活性，呈现出 19 nM 的 IC50 值。Vonoprazan hydrochloride 主要应用于胃酸相关疾病的研究，包括胃食管反流病和消化性溃疡，并可用于根除幽门螺杆菌。

(R)-ND-336 is a highly potent and selective MMP-9 inhibitor, displaying a K i value of 19 nM. It also exhibits inhibitory activity against MMP-2 (K i = 127 nM) and MMP-14 (K i =119 nM). With its significant potential, (R)-ND-336 is being investigated in the field of diabetic foot ulcers (DFUs) research [1].

19-O-Acetylchaetoglobosin A is a fungal metabolite originally isolated fromC. globosumthat has actin polymerization inhibitory and cytotoxic activities.1,2It inhibits actin polymerization in a cell-free assay when used at a concentration of 2 μM.219-O-Acetylchaetoglobosin A (3.2, 10, and 32 μg ml) is cytotoxic to HeLa cervical cancer cells.1 1.Umeda, M., Ohtsubo, K., Saito, M., et al.Cytotoxicity of new cytochalasans from Chaetomium globosumExperientia31(4)435-438(1975) 2.Sekita, S., Yoshihira, K., Natori, S., et al.Structure-activity relationship of thirty-nine cytochalasans observed in the effects on cellular structures and cellular events and on actin polymerization in vitroJ. Pharmacobiodyn.8(11)906-916(1985)

Vonoprazan (TAK-438 (free base)) 是一种质子泵抑制剂，是口服活性钾竞争性酸阻断剂，有抗分泌作用。在 pH 为 6.5 时，它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性，IC50值为 19 nM。它可用于研究胃酸相关疾病。

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

CDK2-IN-19 (Compound 32)为一种口服活性的选择性CDK2抑制剂（Ki：0.18 nM），在带OVCAR3肿瘤的小鼠模型中表现出显著的抗癌效果。

5-HT6 agonist 1 (Compound 19)为一种5-HT6激动剂 (Ki: 5 nM)，展现出抗抑郁样特性并能改善认知缺陷，同时能抑制血小板聚集，具备高代谢稳定性。

Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K., et al.Aquastatin A, an inhibitor of mammalian adenosine triphosphatases from Fusarium aquaeductuum. Taxonomy, fermentation, isolation, structure determination and biological propertiesJ. Antibiot. (Tokyo)46(11)1648-1657(1993) 2.Kwon, Y.-J., Fang, Y., Xu, G.-H., et al.Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611Biol. Pharm. Bull.32(12)2061-2064(2009) 3.Seo, C., Soh, J.H., Oh, H., et al.Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060Bioorg. Med. Chem. Lett.19(21)6095-6097(2009)

A3AR agonist 2 (Compound 19) 是高选择性A3AR激动剂，Ki为22.1 nM。本化合物有效促进β-arrestin2募集，展现出EC50为4.36 nM。A3AR agonist 2 主要用于研究炎症性疾病、缺血、癌症、神经性疼痛、肝脏病以及其他慢性病态。

Antibacterial agent 19 是一种有效的抗菌剂。Antibacterial agent 19 对K. pneumoniae，(M-R)S. aureus 和 (M-R,V-R)S. aureus 具有抗菌活性, 其 MIC 值为 0.022, 0.022 和 0.045 mg/mL。