DC661

製品コードS8808 バッチS880801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₁H₃₉Cl₂N₅
	分子量	552.58	CAS No.	1872387-43-3
Solubility (25°C)*	体外	Ethanol	49 mg/mL (88.67 mM)
		DMSO	7 mg/mL (12.66 mM)
		Water	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	DC661は強力なパルミトイルプロテインチオエステラーゼ1（PPT1）阻害剤です。DC661は、HCQよりもはるかに優れた能力でリソソームを脱酸し、オートファジーを阻害します。DC661はアポトーシスを誘発します。
in vitro	Treatment of melanoma cells with DC661 results in a more striking accumulation of the autophagic vesicle marker LC3B-II at lower concentrations compared with either Lys05 or HCQ, reflecting more pronounced accumulation of autophagic vesicles at concentrations between 0.1 and 10 μmol/L. All cells die at concentrations above 10 μmol/L for this compound in contrast to Lys05 and HCQ. Compared with HCQ or Lys05, this compound treatment induces a significantly more potent inhibition of autophagic flux in melanoma cells expressing the mCherry-eGFP-LC3B reporter, and significantly higher levels of free GFP in melanoma cells expressing GFP-LC3B. This compound treatment resulted in significantly greater lysosomal deacidification compared with either HCQ or Lys05. The IC50 of this chemical in 72-hour MTT assays is 100-fold lower than that of HCQ across multiple cancer cell lines including colon and pancreas cancer cell lines. This compound suppresses long-term clonogenic growth of melanoma cells more effectively and induces significantly more apoptosis than Lys05, HCQ, or combined BRAF and MEK inhibition in BRAF-mutant melanoma cells.
in vivo	Treatment with the reduced dose (3 mg/kg, i.p.) of DC661 in a HT29 xenograft results in a significant reduction in tumor volume and almost complete suppression of daily tumor growth rate compared with control mice without significantly affecting mouse weight.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A375P cells
	濃度	0.1, 0.3, 1, 3, 10 μM
	反応時間	6 hours
	実験の流れ	A375P cells are treated with doses of HCQ, Lys05, or DC661 for 6 hours before lysates are immunoblotted.
動物実験	動物モデル	HT29 colorectal xenograft
	投薬量	3 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/30442709/

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：

The AKT-USP15 axis modulates autophagy in MPP+-induced Parkinson's disease model of SN4741 cells [ Cell Signal, 2025, 134:111879]	PubMed: 40441471
Divergent effects of acute and chronic PPT1 inhibition in melanoma [ Autophagy, 2024, 1-13.]	PubMed: 39265628
E3 ubiquitin ligase TRIM2 identified as a novel suppressor of CYP11B2 and aldosterone production [ Cell Mol Life Sci, 2024, 82(1):27]	PubMed: 39725733
Lysosomal lipid peroxidation regulates tumor immunity [ J Clin Invest, 2023, 133(8)e164596]	PubMed: 36795483
Targeting AKT induced Ferroptosis through FTO/YTHDF2-dependent GPX4 m6A methylation up-regulating and degradating in colorectal cancer [ Cell Death Discov, 2023, 9(1):457]	PubMed: 38102129
ASCL2 Maintains Stemness Phenotype through ATG9B and Sensitizes Gliomas to Autophagy Inhibitor [ Adv Sci (Weinh), 2022, 9(27):e2105938]	PubMed: 35882624
Calenduloside E protects against myocardial ischemia-reperfusion injury induced calcium overload by enhancing autophagy and inhibiting L-type Ca2+ channels through BAG3 [ Biomed Pharmacother, 2022, 145:112432]	PubMed: 34798472
SYVN1-mediated ubiquitination and degradation of MSH3 promotes the apoptosis of lens epithelial cells [ FEBS J, 2022, 10.1111/febs.16447]	PubMed: 35334159
Poly (ADP-ribose) polymerase 1-mediated defective mitophagy contributes to painful diabetic neuropathy in the db/db model [ J Neurochem, 2022, 10.1111/jnc.15606]	PubMed: 35263449
ER proteins decipher the tubulin code to regulate organelle distribution [ Nature, 2021, 10.1038/s41586-021-04204-9]	PubMed: 34912111

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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