LB-100

製品コードS7537 バッチS753702

化学情報

	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は、BxPc-3細胞で0.85 μM、Panc-1細胞で3.87 μMのIC50を示す水溶性のプロテインホスファターゼ2A（PP2A）阻害剤です。
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, this compound reduces the PP2A activity by 30-50%. It increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. This chemical increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.
in vivo	In a mouse pancreatic cancer xenograft model, LB-100 (2 mg/kg, i.p.) enhances chemotherapy of doxorubicin. This compound causes higher density of microvessel in tumors and rapid blood flow at the surface of tumors.

プロトコル(参考用のみ)

キナーゼアッセイ	PP2A activity assays
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/25304380/

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：

PPP2R1A mutations portend improved survival after cancer immunotherapy [ Nature, 2025, 10.1038/s41586-025-09203-8]	PubMed: 40604275
Inter-platelet communication driving thrombus formation is regulated by extracellular calpain-1 cleavage of connexin 62 [ Haematologica, 2025, 110(8):1822-1833]	PubMed: 40045892
RNA polymerase II subunit 5-mediating protein limits TLR4-induced innate immune activation in macrophages by inhibiting IKKβ/NF-κB signaling during sepsis [ Cell Commun Signal, 2025, 23(1):274]	PubMed: 40495190
LB-100 Enhances Drugs Efficacy Through Inhibition of P-Glycoprotein Expression in Multidrug-Resistant Glioblastoma and Non-Small Cell Lung Carcinoma Cellular Models [ Pharmaceutics, 2025, 17(2)189]	PubMed: 40006556
PP2A attenuates α-amanitin-induced liver injury by promoting autophagy and inhibiting apoptosis in mouse models [ Chem Biol Interact, 2025, 417:111558]	PubMed: 40379039
Oncogene Silencing via ecDNA Micronucleation [ bioRxiv, 2025, 2025.04.15.648906]	PubMed: 40321211
CUL4B mutations impair human cortical neurogenesis through PP2A-dependent inhibition of AKT and ERK [ Cell Death Dis, 2024, 15(2):121]	PubMed: 38331954
PTGER4 signaling regulates class IIa HDAC function and SPINK4 mRNA levels in rectal epithelial cells [ Cell Commun Signal, 2024, 22(1):493]	PubMed: 39396982
The immunosuppressive drug cyclosporin A has an immunostimulatory function in CD8+ T cells [ Eur J Immunol, 2024, e2350825.]	PubMed: 38650034
An AMBRA1, ULK1 and PP2A regulatory network regulates cytotoxic T cell differentiation via TFEB activation [ Sci Rep, 2024, 14(1):31838]	PubMed: 39738384

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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