219492
Cdk4/6 Inhibitor IV
The Cdk4/6 Inhibitor IV, also referenced under CAS 359886-84-3, controls the biological activity of Cdk4/6. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
別名:
Cdk4/6 Inhibitor IV, trans-4-((6-(ethylamino)-2-((1-(phenylmethyl)-1H-indol-5-yl)amino)-4-pyrimidinyl)amino)-cyclohexanol, CINK4
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About This Item
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品質水準
アッセイ
≥95% (HPLC)
フォーム
solid
メーカー／製品名
Calbiochem®
保管条件
OK to freeze
protect from light
色
pale amber
溶解性
DMSO: 10 mg/mL
輸送温度
ambient
保管温度
2-8°C
詳細
A cell-permeable triaminopyrimidine compound that acts as a reversible and ATP-competitive inhibitor against Cyclin D1-complexed, but not Cyclin D2-complexed, Cdk4 and Cdk6 (IC50 = 1.5 & 5.6 µM, respectively) with much reduced activity against Cdk5/p35 (IC50 = 25 µM) and little or no activity towards Cdk1/CycB,
Cdk2/CycA, Cdk2/CycE, v-abl, c-met, IGF-1R, or IR (IC50 >10 µM). CINK4 (at 5 & 10 µM) effectively inhibits cellular Cdk4 substrate pRb phosphorylation and prevents serum-stimulated G1/S transition of serum starved pRb-positive, but not pRb-negative, cultures. CINK4 is shown to exert a ~46% suppression of human colon carcinoma HCT116-derived tumor growth in mice in vivo (30 mg/kg; twice a day i.p.).
Cdk2/CycA, Cdk2/CycE, v-abl, c-met, IGF-1R, or IR (IC50 >10 µM). CINK4 (at 5 & 10 µM) effectively inhibits cellular Cdk4 substrate pRb phosphorylation and prevents serum-stimulated G1/S transition of serum starved pRb-positive, but not pRb-negative, cultures. CINK4 is shown to exert a ~46% suppression of human colon carcinoma HCT116-derived tumor growth in mice in vivo (30 mg/kg; twice a day i.p.).
A cell-permeable triaminopyrimidine compound that acts as a reversible and ATP-competitive inhibitor against Cyclin D1-complexed, but not Cyclin D2-complexed, Cdk4 and Cdk6 (IC50 = 1.5 and 5.6 µM, respectively) with much reduced activity against Cdk5/p35 (IC50 = 25 µM) and little or no activity towards Cdk1/CycB, Cdk2/CycA, Cdk2/CycE, v-abl, c-met, IGF-1R, or IR (IC50 >10 µM). CINK4 (at 5 and 10 µM) effectively inhibits cellular Cdk4 substrate pRb phosphorylation and prevents serum-stimulated G1/S transition of serum starved pRb-positive, but not pRb-negative, cultures. CINK4 is shown to exert a ~46% suppression of human colon carcinoma HCT116-derived tumor growth in mice in vivo (30 mg/kg; twice a day, i.p.).
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
その他情報
Soni, R., et al. 2001. J. Natl. Cancer Inst.93, 436.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類コード
11 - Combustible Solids
WGK
WGK 2
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
219492-5MG:
219492-MG:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Clivia Lisowski et al.
Autophagy, 18(8), 1785-1800 (2021-11-17)
Modulation of the host cell cycle has emerged as a common theme among the pathways regulated by bacterial pathogens, arguably to promote host cell colonization. However, in most cases the exact benefit ensuing from such interference to the infection process
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