Tacedinaline (CI994)

製品コードS2818 バッチS281801

化学情報

	Synonyms	PD-123654, GOE-5549, Acetyldinaline	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₁₅N₃O₂
	分子量	269.3	CAS No.	112522-64-2
Solubility (25°C)*	体外	DMSO	54 mg/mL (200.51 mM)
		Water	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	Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.
in vitro	CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells. ^[2] CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. ^[3] CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines. ^[4] CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. ^[5]
in vivo	CI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LNCaP cell lines
	濃度	2.5 μM
	反応時間	2-4 days
	実験の流れ	LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×10⁴) are seeded in 24-well plates and incubated in a 5% CO₂ incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.
動物実験	動物モデル	human prostate tumor model LNCaP
	投薬量	535 mg/kg
	投与方法	Administered via oral gavage

参考

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by , , J Biol Chem, 2016, 291(14):7386-95]

: Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]

: Data from [Data independently produced by , , Int J Biochem Cell Biol, 2016, 81(Pt A):82-91]

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：

CUDC-907, a dual PI3K/histone deacetylase inhibitor, increases meta-iodobenzylguanidine uptake (123/131I-mIBG) in vitro and in vivo: a promising candidate for advancing theranostics in neuroendocrine tumors [ J Transl Med, 2023, 21(1):604]	PubMed: 37679770
Histone deacetylase III interactions with BK polyomavirus large tumor antigen may affect protein stability [ Virol J, 2023, 20(1):155]	PubMed: 37464367
MyoD is a 3D genome structure organizer for muscle cell identity [ Nat Commun, 2022, 13(1):205]	PubMed: 35017543
Development of Human Adrenocortical Adenoma (HAA1) Cell Line from Zona Reticularis [ Int J Mol Sci, 2022, 24(1)584]	PubMed: 36614027
Rb-E2F-HDAC Repressor Complexes Control Interferon-Induced Repression of Adenovirus To Promote Persistent Infection [ J Virol, 2022, e0044222]	PubMed: 35546119
Pre-Senescence Induction in Hepatoma Cells Favors Hepatitis C Virus Replication and Can Be Used in Exploring Antiviral Potential of Histone Deacetylase Inhibitors [ Int J Mol Sci, 2021, 22(9)4559]	PubMed: 33925399
Combination Treatment of CI-994 With Etoposide Potentiates Anticancer Effects Through a Topoisomerase II-Dependent Mechanism in Atypical Teratoid/Rhabdoid Tumor (AT/RT) [ Front Oncol, 2021, 11:648023]	PubMed: 34367950
HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062]	PubMed: 33639591
Protein acetylation derepresses Serotonin Synthesis to potentiate Pancreatic Beta-Cell Function through HDAC1-PKA-Tph1 signaling [ Theranostics, 2020, 10(16):7351-7368]	PubMed: 32641996
Targeted Therapy for mTORC1-driven Tumours Through HDAC Inhibition by Exploiting Innate Vulnerability of mTORC1 Hyper-Activation [ Br J Cancer, 2020, 27]	PubMed: 32336756

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。