Ciliobrevin D

製品コードS9743 バッチS974301

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C17H8Cl3N3O2

分子量 392.62 CAS No. 1370554-01-0
Solubility (25°C)* 体外 DMSO 20 mg/mL (50.93 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 40%PEG300 5%Tween80 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。

1.000mg/ml (2.55mM) Taking the 1 mL working solution as an example, add 50 μL of 20 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 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。

0.250mg/ml (0.64mM) Taking the 1 mL working solution as an example, add 50 μL of 5 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

Ciliobrevin D(化合物5)は、AAA+(多様な細胞活動に関連するATPアーゼ)ATPaseモーターの細胞質ダイニンに対する細胞透過性、可逆的かつ特異的な拮抗薬です。Ciliobrevin Dは一次繊毛の形成を妨げ、ヘッジホッグ(Hh)シグナル伝達を阻害します。

in vitro

Ciliobrevin D inactivate dynein in Sertoli cells. The inactivation of dynein by this compound also perturbs gross disruption of F-actin across the Sertoli cells in vitro. It perturbs protein trafficking within the primary cilium, leading to their malformation and Hedgehog signaling blockade. This chemical also prevents spindle pole focusing, kinetochore-microtubule attachment, melanosome aggregation, and peroxisome motility in cultured cells.

in vivo

Ciliobrevin D inactivate dynein in the testis. The inactivation of dynein by this compound also perturbs gross disruption of F-actin across the seminiferous epithelium in vivo, illustrating there are cross talks between the two cytoskeletons in the testis.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Sertoli cells
濃度 15 µM, 30 µM
反応時間 1 h
実験の流れ

Sertoli cells cultured in vitro on Matrigel-coated bicameral units at 1.0 × 106 cells/cm2 are used for quantifying the transepithelial electrical resistance in ohms (Ω) across the cell epithelium to assess the TJ-barrier function. In brief, each bicameral unit is placed inside the well of a 24-well dish with 0.5 ml F12/DMEM in the apical and the basal compartments. Dynein is inhibited in Sertoli cells on days 3 and 4 using Ciliobrevin D at 15 µM or 30 µM for 1hr, and Sertoli cell TJ-permeability barrier function is monitored daily by quantifying transepithelial electrical resistance across the cell epithelium.

動物実験 動物モデル adult male Sprague-Dawley rats
投薬量 15 µM per testis
投与方法 local injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/22425997/
  • https://pubmed.ncbi.nlm.nih.gov/30016153/

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:

Ciliary IFT-B Transportation Plays an Important Role in Human Endometrial Receptivity Establishment and is Disrupted in Recurrent Implantation Failure Patients [ Cell Prolif, 2025, e13819.] PubMed: 39915276
MI-181 Modulates Cilia Length and Restores Cilia Length in Cells with Defective Shortened Cilia [ ACS Chem Biol, 2024, 19(8):1733-1742] PubMed: 39106364
Localization of a TORC1-eIF4F translation complex during CD8+ T cell activation drives divergent cell fate [ Mol Cell, 2022, S1097-2765(22)00327-6] PubMed: 35597236
LRRK1-mediated NDEL1 phosphorylation promotes cilia disassembly via dynein-2-driven retrograde intraflagellar transport [ J Cell Sci, 2022, 135(21)jcs259999] PubMed: 36254578

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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