受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H17NO3 |
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分子量 | 331.36 | CAS No. | 321674-73-1 | |
Solubility (25°C)* | 体外 | DMSO | 66 mg/mL (199.17 mM) | |
Ethanol | 3 mg/mL (9.05 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells. |
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in vitro | BIBR 1532 exhibits an non-competitive inhibitory effect on telomerase activity. [1] In JVM13 leukemia cell line, BIBR 1532 shows an antiproliferative effect in a dose-dependent range with IC50 of 52 μM, and similar results are also observed in other leukemia cell lines including Nalm-1, HL-60, and Jurkat. In addition, BIBR 1532 results in a direct antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56 μM without affecting the proliferative capacity of normal hematopoietic progenitor cells. [2] BIBR 1532 (2.5 μM) reduces colony-forming ability, and induces telomere length shortening as well as chemotherapeutic sensitization by inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines. [3] In T-cell prolymphocytic leukemia (T-PLL), BIBR 1532 shows selective cytotoxic effects in a dose-dependent manner and BIBR 1532-treated cells also demonstrates nuclear condensation and formation of apoptotic bodies morphologically compatible with apoptosis. [4] A recent study shows that combination treatment of BIBR 1532 and chemotherapeutic agents carboplatin results in a potential synergy for eliminateing ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines. [5] |
キナーゼアッセイ | Conventional Telomerase Assay | |
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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 | ||
細胞アッセイ | 細胞株 | JVM13 |
濃度 | 0 to 80 μM | |
反応時間 | 24 -72 hours | |
実験の流れ | 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. |
Data from [J Mol Neurosci, 2013, 51(1), 187-98]
Data from [Data independently produced by , , Oncotarget, 2017, 8(1):179-190]
A CRISPR base editing approach for the functional assessment of telomere biology disorder-related genes in human health and aging [ Biogerontology, 2024, 10.1007/s10522-024-10094-x] | PubMed: 38310618 |
Telomere dysfunction promotes cholangiocyte senescence and biliary fibrosis in primary sclerosing cholangitis [ JCI Insight, 2023, 10.1172/jci.insight.170320] | PubMed: 37707950 |
Short-Term TERT Inhibition Impairs Cellular Proliferation via a Telomere Length-Independent Mechanism and Can Be Exploited as a Potential Anticancer Approach [ Cancers (Basel), 2023, 15(10)2673] | PubMed: 37345011 |
High-Content and High-Throughput Clonogenic Survival Assay Using Fluorescence Barcoding [ Cancers -Basel), 2023, 15(19)4772] | PubMed: 37835466 |
BIBR1532 inhibits proliferation and enhances apoptosis in multiple myeloma cells by reducing telomerase activity [ PeerJ, 2023, 10.7717/peerj.16404] | PubMed: 37953768 |
Telomerase RNA TERC and the PI3K-AKT pathway form a positive feedback loop to regulate cell proliferation independent of telomerase activity [ Nucleic Acids Res, 2022, gkac179] | PubMed: 35323972 |
TERC suppresses PD-L1 expression by downregulating RNA binding protein HuR [ Sci China Life Sci, 2022, 65(12):2505-2516] | PubMed: 35661964 |
Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres [ Cell Death Dis, 2022, 13(11):1005] | PubMed: 36437244 |
PGC1α Regulates the Endothelial Response to Fluid Shear Stress via Telomerase Reverse Transcriptase Control of Heme Oxygenase-1 [ Arterioscler Thromb Vasc Biol, 2022, 42(1):19-34] | PubMed: 34789002 |
Telomerase and Pluripotency Factors Jointly Regulate Stemness in Pancreatic Cancer Stem Cells [ Cancers (Basel), 2021, 13(13)3145] | PubMed: 34201898 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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