Iadademstat (ORY-1001) 2HCl

製品コードS7795 バッチS779501

化学情報

	Synonyms	RG-6016	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₂₂N₂. 2HCl
	分子量	303.27	CAS No.	1431326-61-2
Solubility (25°C)*	体外	Water	61 mg/mL (201.14 mM)
		DMSO	5 mg/mL (16.48 mM)
		Ethanol	4 mg/mL warmed with 50ºC water bath (13.18 mM)
* <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	Iadademstat 2HCl (ORY-1001, RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.
in vitro	In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells. ^[1]
in vivo	In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NRK-52E cells
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells treated with ORY-1001 (10 μM) for 24 h in the presence (vehicle) or TGF-β1.
動物実験	動物モデル	Rodent MV(4;11) xenografts
	投薬量	<0.020mg/kg
	投与方法	p.o.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Br J Haematol, 2017, doi: 10.1111/bjh.14983]

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：

MAF amplification licenses ERα through epigenetic remodelling to drive breast cancer metastasis [ Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y]	PubMed: 37945904
Pharmacological inhibition of LSD1 suppresses growth of hepatocellular carcinoma by inducing GADD45B [ MedComm (2020), 2023, 4(3):e269]	PubMed: 37250145
E3 ligase Trim35 inhibits LSD1 demethylase activity through K63-linked ubiquitination and enhances anti-tumor immunity in NSCLC [ Cell Rep, 2023, 10.1016/j.celrep.2023.113477]	PubMed: 37979167
Targeting Lysine-Specific Demethylase 1 Rescues Major Histocompatibility Complex Class I Antigen Presentation and Overcomes Programmed Death-Ligand 1 Blockade Resistance in SCLC [ J Thorac Oncol, 2022, 17(8):1014-1031]	PubMed: 35691495
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7]	PubMed: 35332332
Targeting histone demethylase LSD1 for treatment of deficits in autism mouse models [ Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8]	PubMed: 35296809
Loss-of-function variants in the schizophrenia risk gene SETD1A alter neuronal network activity in human neurons through the cAMP/PKA pathway [ Cell Rep, 2022, 39(5):110790]	PubMed: 35508131
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity [ J Enzyme Inhib Med Chem, 2022, 37(1):973-985]	PubMed: 35317680
Targeting lysine-specific demethylase 1A inhibits renal epithelial-mesenchymal transition and attenuates renal fibrosis [ FASEB J, 2022, 36(1):e22122]	PubMed: 34958158
The metabesity factor HMG20A potentiates astrocyte survival and reactive astrogliosis preserving neuronal integrity [ Theranostics, 2021, 11(14):6983-7004]	PubMed: 34093866

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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