SMER3

製品コードS4925 バッチS492502

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₁H₄N₄O₂

分子量

224.18

CAS No.

67200-34-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

15 mg/mL (66.91 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.150mg/ml (0.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.550mg/ml (2.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	SMER3, the small-molecule enhancer of rapamycin (SMER), is an inhibitor of the Skp1-Cullin-F-box (SCF)^Met30 ubiquitin ligase with IC50 of 51 nM.
in vitro	SMER3 specifically inhibits ubiquitination by recombinant reconstituted SCF^Met30, selectively disassembles or prevents assembly of SCF^Met30 but not other SCF complexes, and directly binds to Met30 (or Met30-Skp1 complex), but not Skp1 alone, which inhibits Met30 bounding to Skp1. This compound treatment is able to upregulate a set of methionine biosynthesis genes. It enhances rapamycin’s growth inhibitory effect by inhibition of SCF^Met30 and blocking Met4 ubiquitination. ^[1]

製品説明

SMER3, the small-molecule enhancer of rapamycin (SMER), is an inhibitor of the Skp1-Cullin-F-box (SCF)^Met30 ubiquitin ligase with IC50 of 51 nM.

in vitro

SMER3 specifically inhibits ubiquitination by recombinant reconstituted SCF^Met30, selectively disassembles or prevents assembly of SCF^Met30 but not other SCF complexes, and directly binds to Met30 (or Met30-Skp1 complex), but not Skp1 alone, which inhibits Met30 bounding to Skp1. This compound treatment is able to upregulate a set of methionine biosynthesis genes. It enhances rapamycin’s growth inhibitory effect by inhibition of SCF^Met30 and blocking Met4 ubiquitination. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	SCF E3 ligase assay
キナーゼアッセイ	^GstSkp1, Cdc53, ^6xHisMet30 and Rbx1 are co-expressed in Hi5 cells and SCF^Met30 is purified on glutathione sepharose. Recombinant ^FLAG-6xHisMet4 is bound to SCF^Met30 and the ligase/substrate complex is eluted with glutathione. Sic1 in vitro ubiquitination by recombinant SCF^Cdc4 is performed. To directly compare the effect of SMER3 on SCF^Met30 and SCF^Cdc4, Met4 and Sic1 ubiquitination are assayed in a single reaction. Approximately 150 nM SCF^Met30 and SCF^Cdc4 are incubated with DMSO (solvent control) or this compound for 20 min at 25 ℃. The reaction is started by addition of a final concentration of 250 nM yeast E1, 0.8 μM recombinant Cdc34 purified from E. coli36, 5 mM ATP, and 80 μM ubiquitin. Reactions are incubated at 30 ℃ and samples are taken after 5 min and 25 min reaction time to accommodate different reaction kinetics by the two SCFs. Products are separated on SDS-PAGE and analyzed by immunoblotting using anti-Met4 and anti-Sic1 antibodies.

参考

https://pubmed.ncbi.nlm.nih.gov/20581845/

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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