Thiomyristoyl

別名：TM

製品コード：S8245 純度：99.84%

Thiomyristoyl (TM) is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.

CAS No. 1429749-41-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 52300	国内在庫なし(納期7~10日)
2mg	JPY 22000	国内在庫あり
5mg	JPY 40500	国内在庫あり
25mg	JPY 130500	国内在庫あり
100mg	JPY 295500	国内在庫なし(納期7~10日)
1g	JPY 748500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（6）

製品安全説明書

現在のバッチを見る： S824501 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] true] Water] Insoluble] false 純度： 99.84%

99.84

Thiomyristoyl関連製品

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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

Sirtuinシグナル伝達経路

Sirtuin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HeLa	Cytotoxicity assay	50 uM	72 hrs	Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 50 uM measured after 72 hrs by CCK8 assay	31117516
MCF7	Growth inhibition assay	15 uM	72 hrs	Growth inhibition of human MCF7 cells at 15 uM measured after 72 hrs by AlamarBlue assay	31144814
Neuro2a	Function assay	0.2 to 2 uM	24 hrs	Induction of neurite outgrowth in mouse Neuro2a cells at 0.2 to 2 uM measured after 24 hrs by microscopic analysis	31144814
HCT116	Function assay	25 uM	6 hrs	Inhibition of SIRT2 in human HCT116 cells assessed as increase in alpha-tubulin acetylation at 25 uM incubated for 6 hrs by DAPI staining-based laser scanning confocal microscopic analysis	30986062
HCT116	Function assay	50 uM	6 hrs	Inhibition of SIRT2 in human HCT116 cells assessed as increase in alpha-tubulin acetylation at 50 uM incubated for 6 hrs by DAPI staining-based laser scanning confocal microscopic analysis	30986062
BxPC3	Growth inhibition assay		72 hrs	Growth inhibition of human BxPC3 cells after 72 hrs by CellTiter-Blue assay, GI50=13.3μM	30986062
MDA-MB-468	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-468 cells after 72 hrs by CellTiter-Blue assay, GI50=15.7μM	30986062
NCI-H23	Growth inhibition assay		72 hrs	Growth inhibition of human NCI-H23 cells after 72 hrs by CellTiter-Blue assay, GI50=16.4μM	30986062
HCT116	Function assay		5 days	Inhibition of anchorage-independent cell growth in human HCT116 cells assessed as reduction in colony formation incubated for 5 days followed by compound re-addition and measured after 9 to 11 days by nitro blue tetrazolium chloride-based soft agar colony, GI50=16.7μM	30986062
A549	Growth inhibition assay		72 hrs	Growth inhibition of human A549 cells after 72 hrs by CellTiter-Blue assay, GI50=17.3μM	30986062
SW948	Growth inhibition assay		72 hrs	Growth inhibition of human SW948 cells after 72 hrs by CellTiter-Blue assay, GI50=19.2μM	30986062
MCF7	Growth inhibition assay		72 hrs	Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay, GI50=37μM	30986062
MDA-MB-231	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay, GI50=42.8μM	30986062
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Thiomyristoyl (TM) is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.

Targets

SIRT2 ^[1]
(Cell-free assay)

28 nM

In Vitro
In vitro	Thiomyristoyl(TM) is a highly selective SIRT2 inhibitor. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7. In vitro, it shows great inhibition of cell viability and its cytotoxicity is relatively selective toward cancer cells. TM decreases c-Myc oncoprotein level in cancer cells, the ability of TM to decrease c-Myc abundance in different cell lines correlates with the sensitivity of the cell lines to TM^[1].
細胞実験	細胞株	breast cancer cell lines MCF-7
	濃度	1, 5, 10, 25, 50 μM
	反応時間	6 h
	実験の流れ	Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control.

In Vivo
In Vivo	The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM has limited effects on non-cancerous cells and tumor-free mice^[1].
動物実験	動物モデル	Mouse xenograft model
	投与量	1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT)
	投与経路	intraperitoneal (IP) or intra-tumor (IT) injections

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06133153	Not yet recruiting	Lip; Anomaly	Croma-Pharma GmbH\|Proinnovera GmbH	March 2024	Not Applicable
NCT06147232	Not yet recruiting	Nephropathy\|Diabetic Nephropathies\|Diabetes Mellitus Type 1\|Albuminuria\|Diabetic Complications Renal\|Diabetic Complications Cardiovascular\|Hypoxia	Steno Diabetes Center Copenhagen\|Juvenile Diabetes Research Foundation\|King''s College London\|Glostrup University Hospital Copenhagen	February 2024	Phase 4
NCT05505643	Not yet recruiting	Breast Cancer\|Breast Neoplasm	Washington University School of Medicine\|The Foundation for Barnes-Jewish Hospital\|Varian Medical Systems	February 28 2024	Not Applicable
NCT05134740	Recruiting	Hodgkins Lymphoma\|Non Hodgkins Lymphoma	Baylor College of Medicine\|Center for Cell and Gene Therapy Baylor College of Medicine	January 2024	Phase 1

参考
[1] Jing H, et al. Cancer Cell. 2016, 29(3):297-310.

参考

[1] Jing H, et al. Cancer Cell. 2016, 29(3):297-310.

化学情報

分子量	581.85	化学式	C₃₄H₅₁N₃O₃S
CAS No.	1429749-41-6	SDF	Download Thiomyristoyl SDFをダウンロードする
Smiles	CCCCCCCCCCCCCC(=S)NCCCCC(C(=O)NC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (171.86 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):