Lys05

Catalog No.S8369 Batch:S836901

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Technical Data

Formula

C23H23Cl2N5.3HCl
Molecular Weight 549.75 CAS No. 1391426-24-6
Solubility (25°C)* In vitro DMSO 9 mg/mL (16.37 mM)
Water 3 mg/mL (5.45 mM)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
Autophagy [1]
In vitro

Lys05 is water soluble salt of Lys01. Lys05 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 Lys05 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, Lys05 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 Lys05 or chronic daily dosing of Lys05 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].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Nu/Nu nude mice

  • Dosages

    10 mg/kg, 40 mg/kg, or 80 mg/kg

  • Administration

    i.p.

Selleck's Lys05 has been cited by 9 publications

Targeting autophagy as a therapeutic strategy in pediatric acute lymphoblastic leukemia [ Sci Rep, 2024, 14(1):4000] PubMed: 38369625
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
The combination of CUDC-907 and gilteritinib shows promising in vitro and in vivo antileukemic activity against FLT3-ITD AML [ Blood Cancer J, 2021, 11(6):111] PubMed: 34099621
Faciogenital dysplasia 5 confers the cancer stem cell-like traits of gastric cancer cells through enhancing Sox2 protein stability [ Environ Toxicol, 2021, 10.1002/tox.23355] PubMed: 34427968
Inhibition of autophagy mitigates cell migration and invasion in thyroid cancer [ Surgery, 2021, S0039-6060(21)00795-9] PubMed: 34565609
Autophagy promotes osteoclast podosome disassembly and cell motility athrough the interaction of kindlin3 with LC3. [ Cell Signal, 2020, 67:109505] PubMed: 31857241

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.