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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 | C17H13Br2N5OS.HBr |
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分子量 | 576.10 | CAS No. | 1217022-63-3 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL warmed with 50ºC water bath (173.58 mM) | |
Water | Insoluble | |||
Ethanol | 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 | PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs). |
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in vitro | PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1] |
in vivo | PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1] |
特徴 | BMI-1-selective inhibitor, targeting the BMI-1 self-renewal machinery. |
キナーゼアッセイ | Untranslated region-mediated luciferase reporter expression | |
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HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control. | ||
細胞アッセイ | 細胞株 | Human lymphoma U937 and HT1080 tumor cells, primary human peripheral blood mononuclear cells and human hematopoietic stem cells. |
濃度 | ~10 μM | |
反応時間 | 4 days | |
実験の流れ | To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment. | |
動物実験 | 動物モデル | Primary human colon cancer xenograft, human colon cancer cell lines LIM1215 and HCT116 xenografts in nude mice. |
投薬量 | ~60 mg/kg/day | |
投与方法 | s.c. |
Data from [Data independently produced by , , J Hematol Oncol, 2016, 9:17]
Data from [Data independently produced by , , Oncotarget, 2016, 7(1):745-58]
Data from [Data independently produced by , , Cell Cycle, 2018, 17(10):1199-1211]
Cathepsin-facilitated invasion of BMI1-high hepatocellular carcinoma cells drives bile duct tumor thrombi formation [ Nat Commun, 2023, 10.1038/s41467-023-42930-y] | PubMed: 37923799 |
BMI1 promotes spermatogonial stem cell maintenance by epigenetically repressing Wnt10b/β-catenin signaling [ Int J Biol Sci, 2022, 18(7):2807-2820] | PubMed: 35541907 |
PRC1-independent binding and activity of RYBP on the KSHV genome during de novo infection [ PLoS Pathog, 2022, 18(8):e1010801] | PubMed: 36026503 |
BMI1 promotes osteosarcoma proliferation and metastasis by repressing the transcription of SIK1 [ Cancer Cell Int, 2022, 22(1):136] | PubMed: 35346195 |
Identification of a novel binding inhibitor that blocks the interaction between hSCARB2 and VP1 of enterovirus 71 [ Cell Insight, 2022, 1(2):100016] | PubMed: 37193133 |
BMI1 Drives Steroidogenesis Through Epigenetically Repressing the p38 MAPK Pathway [ Front Cell Dev Biol, 2021, 9:665089] | PubMed: 33928089 |
BMI1 promotes spermatogonia proliferation through epigenetic repression of Ptprm [ Biochem Biophys Res Commun, 2021, 583:169-177] | PubMed: 34739857 |
Polycomb group protein Bmi1 is required for the neuronal differentiation of mouse induced pluripotent stem cells [ Exp Ther Med, 2021, 21(6):619] | PubMed: 33936276 |
BMI1 promotes steroidogenesis through maintaining redox homeostasis in mouse MLTC-1 and primary Leydig cells [ Cell Cycle, 2020, 19(15):1884-1898] | PubMed: 32594840 |
Hsp70/Bmi1-FoxO1-SOD Signaling Pathway Contributes to the Protective Effect of Sound Conditioning against Acute Acoustic Trauma in a Rat Model [ Neural Plast, 2020, 2020:8823785] | PubMed: 33082778 |
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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