| 名稱 | BIBR 1532 |
| 描述 | BIBR 1532 is an effective, specific and non-competitive telomerase inhibitor (IC50: 100 nM, in a cell-free assay). |
| 細(xì)胞實(shí)驗(yàn) | Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation. (Only for Reference) |
| 激酶實(shí)驗(yàn) | Conventional Telomerase Assay : For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract is mixed with different concentrations of BIBR1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture is added, and the reaction is initiated by transferring the tubes to 37 °C. The final concentrations in the reaction mixture are 25 mM Tris-Cl (pH 8.3), 1 mM MgCl2, 1 mM EGTA, 1 mM dATP, 1 mM dTTP, 6.3 μM cold dGTP, 15 μCi [α-32P]dGTP (3000 Ci/mmol; NEN), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5 |
| 體內(nèi)活性 | 在MCF-7/WT和抗美法侖的MCF-7/MlnR 細(xì)胞系中,BIBR 1532（2.5 μM）通過(guò)抑制端粒酶活性降低形成集落的能力,并縮短端粒長(zhǎng)度,且誘導(dǎo)對(duì)化療增敏。在體外,BIBR 1532劑量依賴性地非競(jìng)爭(zhēng)性抑制端粒酶活性（IC50：100 nM）。BIBR 1532對(duì)T細(xì)胞幼淋巴細(xì)胞白血病具有選擇性細(xì)胞毒性,該毒性具有劑量依賴性,BIBR 1532處理過(guò)的細(xì)胞也出現(xiàn)核濃縮及凋亡小體形成現(xiàn)象。在JVM13白血病細(xì)胞系中,BIBR 1532具有劑量依賴性的抗增殖效果（IC50：52 μM）,且對(duì)其他白血病細(xì)胞系,包括 Nalm-1,HL-60和Jurkat的結(jié)果相似。此外, 在急性髓細(xì)胞性白血病中,BIBR 1532具有抗增殖效果（IC50：56 μM）,而且不影響正常造血干細(xì)胞的增殖能力。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 21.67 mg/mL (65.39 mM)
Ethanol : 8.3 mg/mL (25 mM)
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| 關(guān)鍵字 | inhibit | BIBR 1532 | Inhibitor | Apoptosis | Telomerase | BIBR-1532 | BIBR1532 |
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| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 抗衰老化合物庫(kù) | 高選擇性抑制劑庫(kù) | NO PAINS 化合物庫(kù) | DNA 損傷和修復(fù)分子庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 共價(jià)抑制劑庫(kù) |