{"product_id":"bisindolylmaleimide-iii-bhb21900415","title":"Bisindolylmaleimide III","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eInhibitors\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eBisindolylmaleimide III is an inhibitor of protein kinase C (PKC), with IC\u003csub\u003e50\u003c\/sub\u003e values of 0.26 μM, 5.7 μM, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. It also inhibits several off-targets, with IC\u003csub\u003e50\u003c\/sub\u003e values of 0.17 μM, 1 μM, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively, and a K\u003csub\u003ei\u003c\/sub\u003e of 16.5 μM for NQO2. The compound selectively binds activated Rsk1 following EGF stimulation and can be used to detect the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK, in studies of signal transduction and colorectal cancer\u003csup\u003e[1][2][3]\u003c\/sup\u003e. It is supplied as a brown to reddish brown solid (C23H20N4O2, MW 384.43) at 98.95% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e137592-43-9\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC23H20N4O2\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e384.43 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e98.95%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eBrown to reddish brown\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eO=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003ePKCα, PKCδ, PKCμ, cdk2\/cyclin A, NQO2\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eEpigenetics; TGF-beta\/Smad; Cytoskeleton; Metabolic Enzyme\/Protease; Neuronal Signaling; Cell Cycle\/DNA Damage\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: 25 mg\/mL (65.03 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003ePowder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003ch3 style=\"font-size:16px;font-weight:700;color:#003366;margin:16px 0 8px\"\u003eIC50 \u0026amp; Target\u003csup\u003e[1]\u003c\/sup\u003e\n\u003c\/h3\u003e\n\u003cp\u003e\u003c\/p\u003e\n\u003ctable\u003e\u003ctbody\u003e\u003ctr\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePKCα\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.26 μM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePKCδ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e5.7 μM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePKCμ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e6 μM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ecdk2\/cyclin A\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e1 μM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eNQO2\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e16.5 μM (Ki)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003c\/tr\u003e\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description and in the In Vitro \u0026amp; In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/14769951\"\u003eBrehmer D, et al. Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors. Molecular \u0026amp; cellular proteomics: MCP. 2004 May;3(5):490-500.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/10432224\"\u003eSaito Y, et al. Role of ecto-kinase in phorbol ester-enhanced growth hormone-binding protein release from human IM-9 cells. Molecular and cellular endocrinology. 1999 Jun 25;152(1-2):65-72.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [3]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/18347986\"\u003ePajak B, et al. Bisindolylmaleimide IX facilitates extrinsic and initiates intrinsic apoptosis in TNF-alpha-resistant human colon adenocarcinoma COLO 205 cells. Apoptosis: an international journal on programmed cell death. 2008 Apr;13(4):509-22.\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"5 mg","offer_id":67604866433389,"sku":"HY-117393-5MG","price":180.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605079032173,"sku":"HY-117393-10MG","price":288.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605079064941,"sku":"HY-117393-50MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605079097709,"sku":"HY-117393-100MG","price":0.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-117393.gif?v=1790972900","url":"https:\/\/www.ebiohippo.com\/products\/bisindolylmaleimide-iii-bhb21900415","provider":"BioHippo","version":"1.0","type":"link"}