Lys05

製品コードS8369 バッチS836901

印刷

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

C₂₃H₂₃Cl₂N₅.3HCl

分子量

549.75

CAS No.

1391426-24-6

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

9 mg/mL (16.37 mM)

Water (warmed with 50ºC water bath)

3 mg/mL (5.45 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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	Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
in vitro	Lys05 is water soluble salt of Lys01. This compound shows potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models^[1]. Lys01 and this chemical produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay^[2].
in vivo	While lower doses of Lys05 are well tolerated and associated with antitumor activity, at the highest dose tested, this compound produces Paneth cell dysfunction and intestinal toxicity, similar to what can be observed in mice and humans with genetic defects in the autophagy gene ATG16L1. In two melanoma xenograft models and a colon cancer xenograft model, intermittent high dose or chronic daily dosing of this chemical at lower doses produces significant early blockade of autophagy in vivo, and has single-agent antitumor activity at doses as low as 10 mg/kg i.p. daily^[1].

製品説明

Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.

in vitro

Lys05 is water soluble salt of Lys01. This compound shows potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models^[1].

Lys01 and this chemical produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay^[2].

in vivo

While lower doses of Lys05 are well tolerated and associated with antitumor activity, at the highest dose tested, this compound produces Paneth cell dysfunction and intestinal toxicity, similar to what can be observed in mice and humans with genetic defects in the autophagy gene ATG16L1. In two melanoma xenograft models and a colon cancer xenograft model, intermittent high dose or chronic daily dosing of this chemical at lower doses produces significant early blockade of autophagy in vivo, and has single-agent antitumor activity at doses as low as 10 mg/kg i.p. daily^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MOLM-13 cells
	濃度
	反応時間	24 h
	実験の流れ
動物実験	動物モデル	Nu/Nu nude mice
	投薬量	10 mg/kg, 40 mg/kg, or 80 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/22878685/
https://pubmed.ncbi.nlm.nih.gov/22566612/
https://pubmed.ncbi.nlm.nih.gov/34099621/

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：

Targeting USP8 causes synthetic lethality through degradation of FGFR2 in ARID1A-deficient ovarian clear cell carcinoma [ NPJ Precis Oncol, 2025, 9(1):69]	PubMed: 40074856
Rapid hepatitis C virus replication machinery removal after antiviral treatment with DAA monitored by multimodal imaging [ Structure, 2025, S0969-2126(25)00193-5]	PubMed: 40553718
In vivo manipulation of the protein homeostasis network in rhabdomyosarcoma [ Oncotarget, 2025, 16:681-696]	PubMed: 40879698
Apolipoprotein E aggregation in microglia initiates Alzheimer's disease pathology by seeding β-amyloidosis [ Immunity, 2024, 57(11):2651-2668.e12]	PubMed: 39419029
Targeting autophagy as a therapeutic strategy in pediatric acute lymphoblastic leukemia [ Sci Rep, 2024, 14(1):4000]	PubMed: 38369625
Autophagy inhibition induces AML cell death and enhances the efficacy of chemotherapy under hypoxia [ bioRxiv, 2024, 2024.11.24.625107]	PubMed: 39651164
ADAR1 downregulation by autophagy drives senescence independently of RNA editing by enhancing p16INK4a levels [ Nat Cell Biol, 2022, 24(8):1202-1210]	PubMed: 35851616
ASCL2 Maintains Stemness Phenotype through ATG9B and Sensitizes Gliomas to Autophagy Inhibitor [ Adv Sci (Weinh), 2022, 9(27):e2105938]	PubMed: 35882624
Targeting euchromatic histone lysine methyltransferases sensitizes colorectal cancer to histone deacetylase inhibitors [ Int J Cancer, 2022, 151(9):1586-1601]	PubMed: 35666536
Trabectedin induces ferroptosis via regulation of HIF-1α/IRP1/TFR1 and Keap1/Nrf2/GPX4 axis in non-small cell lung cancer cells [ Chem Biol Interact, 2022, 369:110262]	PubMed: 36396105

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。