LB-100

製品コードS7537 バッチS753702

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H20N2O4
分子量 268.31 CAS No. 1632032-53-1
Solubility (25°C)* 体外 Water 54 mg/mL (201.25 mM)
DMSO 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
in vitro LB-100 inhibits the cell growth with IC50 of 2.3 μM (in BxPc-3) or 1.7 μM (in Panc-1 cell). In BxPc-3, Panc-1, and SW1990 cells, LB-100 reduces the PP2A activity by 30-50%. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.[1]
in vivo In a mouse pancreatic cancer xenograft model, LB-100 (2 mg/kg, i.p.) enhances chemotherapy of doxorubicin. LB-100 causes higher density of microvessel in tumors and rapid blood flow at the surface of tumors. [1]

プロトコル(参考用のみ)

キナーゼアッセイ PP2A activity assays
Cultured pancreatic cancer cells are treated with IC50 of LB-100 for each cell line or equal volume of vehicle for 2 hours, and PP2A activity assays are then performed using Ser/Thr phosphatase assay kit. Cells are lysed with an ultrasonic cell disruptor, and the PP2A concentration is measured using a Ser/Thr phosphatase assay kit according to the instructions. Assays for each cell line are performed in triplicate.
細胞アッセイ 細胞株 BxPc-3, and Panc-1 cell lines
濃度 ~ 10 μM
反応時間 48 h
実験の流れ

Cytotoxicity is conducted by using a Cell Counting Kit-8. Cells are seeded in 96-well plates with a density of 3000 cells per well and are assessed after treatments following the CCK-8 protocol. Relative cytotoxicity is expressed as a percentage of specific controls.
動物実験 動物モデル BALB/c nude mice bearing Panc-1 xenograft
投薬量 2 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Exp Mol Med, 2018, 50(7):83]

Data from [Data independently produced by , , Am J Pathol, 2017, 187(8):1736-1749]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CUL4B mutations impair human cortical neurogenesis through PP2A-dependent inhibition of AKT and ERK [ Cell Death Dis, 2024, 15(2):121] PubMed: 38331954
Targeting PP2A-dependent autophagy enhances sensitivity to ruxolitinib in JAK2V617F myeloproliferative neoplasms [ Blood Cancer J, 2023, 13(1):106] PubMed: 37423955
VPA mediates bidirectional regulation of cell cycle progression through the PPP2R2A-Chk1 signaling axis in response to HU [ Cell Death Dis, 2023, 14(2):114] PubMed: 36781846
N-acetyltransferase 10 promotes cutaneous wound repair via the NF-κB-IL-6 axis [ Cell Death Discov, 2023, 9(1):324] PubMed: 37644005
The CIP2A-TOPBP1 complex safeguards chromosomal stability during mitosis [ Nat Commun, 2022, 13(1):4143] PubMed: 35842428
LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis [ Adv Sci (Weinh), 2022, e2204522] PubMed: 36161785
Targeting Ribonucleotide Reductase Induces Synthetic Lethality in PP2A-Deficient Uterine Serous Carcinoma [ Cancer Res, 2022, 82(4):721-733] PubMed: 34921012
A cannabidiol aminoquinone derivative activates the PP2A/B55α/HIF pathway and shows protective effects in a murine model of traumatic brain injury [ J Neuroinflammation, 2022, 19(1):177] PubMed: 35810304
PTEN/AKT signaling pathway related to hTERT downregulation and telomere shortening induced in Toxoplasma GRA16-expressing colorectal cancer cells [ Biomed Pharmacother, 2022, 153:113366] PubMed: 35810694
Cytoplasmic zinc promotes IL-1β production by monocytes and macrophages through mTORC1-induced glycolysis in rheumatoid arthritis [ Sci Signal, 2022, 15(716):eabi7400] PubMed: 35015571

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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