Bis-T-23 Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	Bis-T-23 is a promoter of actin-dependent dynamin oligomerization, an HIV-I integrase inhibitor, and a Telstar derivative. Bis-T-23 promotes actin-dependent dynamin oligomerization. Bis-T-23 can be used in studies of HIV and chronic kidney disease (CKD).
In vitro	Bis-T-23（AG1717）（0.18 μM）抑制HIV-1整合酶。[5] AG1717（2 μM）阻止整合酶与底物DNA的结合。[5]
In vivo	Bis-T-23（1 ng）通过靶向足细胞中依赖肌动蛋白的kinesin聚合作用，促进正常的肾小球滤过屏障（GFB）功能。[6] 同时，Bis-T-23（i.p.；20, 40 mg/kg）通过改变肌动蛋白动力学，有效改善蛋白尿症状。[6] 此外，Bis-T-23（i.p.；20, 40 mg/kg）在多种遗传性及慢性肾小球疾病的啮齿动物模型上，能缓解或预防蛋白尿并减少类囊体基质扩张。[6]
Synonyms	Bis T-23, Bis-T 23, AG1717
molecular weight	480.43
Molecular formula	C23H20N4O8
CAS	171674-76-3
Storage	\|Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	H2O: Insoluble DMSO: 12.01 mg/ml (25 mM)
References	1. Sever S, Schiffer M. Actin dynamics at focal adhesions: a common endpoint and putative therapeutic target for proteinuric kidney diseases. Kidney Int. 2018 Jun ; 93(6):1298-1307. doi: 10.1016/j.kint.2017.12.028. Epub 2018 Apr 17. Review. PubMed PMID: 29678354 ; PubMed Central PMCID: PMC5967993. 2. Ono S, Kume S, Yasuda-Yamahara M, Yamahara K, Takeda N, Chin-Kanasaki M, Araki H, Sekine O, Yokoi H, Mukoyama M, Uzu T, Araki SI, Maegawa H. O-linked β-N-acetylglucosamine modification of proteins is essential for foot process maturation and survival in podocytes. Nephrol Dial Transplant. 2017 Sep 1 ; 32(9):1477-1487. doi: 10.1093/ndt/gfw463. PubMed PMID: 28339907. 3. Gu C, Lee HW, Garborcauskas G, Reiser J, Gupta V, Sever S. Dynamin Autonomously Regulates Podocyte Focal Adhesion Maturation. J Am Soc Nephrol. 2017 Feb ; 28(2):446-451. doi: 10.1681/ASN.2016010008. Epub 2016 Jul 18. PubMed PMID: 27432739 ; PubMed Central PMCID: PMC5280009. 4. Del Nogal-Avila M, Donoro-Blazquez H, Saha MK, Marshall CB, Clement LC, Macé CE, Chugh SS. Novel therapeutic approaches for chronic kidney disease due to glomerular disorders. Am J Physiol Renal Physiol. 2016 Jul 1 ; 311(1):F63-5. doi: 10.1152/ajprenal.00245.2016. Epub 2016 May Review. PubMed PMID: 27147672 ; PubMed Central PMCID: PMC4967169. 5. Mazumder A, et al. Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase. Biochemistry. 1995 Nov 21;34(46):15111-22. 6. Schiffer M, et al. Pharmacological targeting of actin-dependent dynamin oligomerization ameliorates chronic kidney disease in diverse animal models. Nat Med. 2015 ; 21(6):601-609.

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Bis-T-23

CAS No.: 171674-76-3