{"product_id":"bi-2536-dual-plk-brd4-inhibitor-destabilizes-myc-tbi4121","title":"BI-2536, Dual Plk\/BRD4 inhibitor; Destabilizes Myc","description":"\u003cp\u003e\u003cspan style=\"font-size: 18px\"\u003e\u003cstrong\u003e\u003cu\u003eProduct Details\u003c\/u\u003e\u003c\/strong\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormal Name: \u003c\/strong\u003e4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eMolecular Formula:\u003c\/strong\u003e C\u003csub\u003e28\u003c\/sub\u003eH\u003csub\u003e39\u003c\/sub\u003eN\u003csub\u003e7\u003c\/sub\u003eO\u003csub\u003e3\u003c\/sub\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormula Weight:\u003c\/strong\u003e 521.67\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 755038-02-9\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003ePurity: \u003c\/strong\u003e\u0026gt;97%\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormulation:\u003c\/strong\u003e powder\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e Soluble in DMSO (up to 20 mg\/ml) or in Ethanol (up to 25 mg\/ml)\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eStorage:\u003c\/strong\u003e -20°C\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eStability:\u003c\/strong\u003e ≥ 1 year.\u003c\/p\u003e\n\u003cp\u003e \u003c\/p\u003e\n\u003cp\u003e\u003cspan style=\"font-size: 18px\"\u003e\u003cstrong\u003e\u003cu\u003eApplications\u003c\/u\u003e\u003c\/strong\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003eDual Plk\/BRD4 inhibitor;  Destabilizes Myc\u003c\/p\u003e\n\u003cp\u003e \u003c\/p\u003e\n\u003cp\u003e\u003cspan style=\"font-size: 18px\"\u003e\u003cstrong\u003e\u003cu\u003eFunctions\u003c\/u\u003e\u003c\/strong\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003eBI 2536 was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective Polo-like kinase inhibitor (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) that caused mitotic arrest and apoptosis induction in various human cancer cell lines. It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells. BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.\u003c\/p\u003e\n\u003cp\u003e \u003c\/p\u003e\n\u003cp\u003e\u003cspan style=\"font-size: 18px\"\u003e\u003cstrong\u003e\u003cu\u003eApplication Procedures\u003c\/u\u003e\u003c\/strong\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003eFirst dissolved in DMSO (up to 20 mg\/ml) or in Ethanol (up to 25 mg\/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.\u003c\/p\u003e\n\u003cp\u003e\u003c!--TBI4121-5MG TBI4121-25MG--\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan style=\"font-size: 13px; font-weight: 700; text-transform: uppercase;\"\u003e\u003cstrong\u003eResearch use only.\u003c\/strong\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003ch2\u003eDocuments\u003c\/h2\u003e\n\u003cul\u003e\u003cli\u003e\u003ca href=\"https:\/\/tribioscience.com\/wp-content\/uploads\/2023\/08\/TBI4121_Data_Sheet.pdf\"\u003eDatasheet (PDF)\u003c\/a\u003e\u003c\/li\u003e\u003c\/ul\u003e","brand":"TriBioScience","offers":[{"title":"5 mg","offer_id":45986667233359,"sku":"TBI4121-5MG","price":616.0,"currency_code":"ILS","in_stock":true},{"title":"25 mg","offer_id":45986667266127,"sku":"TBI4121-25MG","price":2255.0,"currency_code":"ILS","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0712\/0748\/5519\/files\/TBI4121.png?v=1782816255","url":"https:\/\/www.danyel.co.il\/products\/bi-2536-dual-plk-brd4-inhibitor-destabilizes-myc-tbi4121","provider":"danyel biotech","version":"1.0","type":"link"}