Thalidomide-5-OH

Name: Thalidomide-5-OH
Brand: TargetMol
SKU: T9291
Price: 99 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 98.94%

货号 T9291Cas号 64567-60-8

别名 4 - 羟基沙利度胺, 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) 是基于 Thalidomide 的的cereblon 配体，可用于募集CRBN 蛋白。它能够利用 linker 与靶蛋白配体连接，得到 PROTAC 分子。

Thalidomide-5-OH

一键复制产品信息

很棒

纯度: 98.94%

货号 T9291 别名 4 - 羟基沙利度胺, 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dioneCas号 64567-60-8

规格	价格	库存	数量
500 mg	¥ 99	现货
1 mL x 10 mM (in DMSO)	¥ 99	现货

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产品介绍

Thalidomide-5-OH AI Summary

Thalidomide-5-OH exhibits inhibitory activity against tubulin polymerization at 50 μM, with an inhibition rate of 32.0%. It shows significant antiangiogenic properties by inhibiting tube formation in VEGF-induced HUVEC cells at 100 μM, resulting in a 26.0% inhibition. This compound also demonstrates cytotoxicity against various cancer cell lines, including KB, MCF7, IM9, and HS-Sultan, at 100 μg/mL after 72 hours. Additionally, it exhibits a cell proliferation inhibition rate of 93.0% on the human leukemia cell line HL-60, at a concentration of 1*E-5 M, along with a 2.0% NBT positivity against the same cell line. Furthermore, Thalidomide-5-OH displays bioactivities related to PROTAC (Proteolysis Targeting Chimera) at CRBN/GSPT1, where it induces degradation of GSPT1 in human MOLT-4 cells. It shows an IC50 value of 376.0 nM for displacing fluorescent tracer from NanoLuc-tagged CRBN, achieving a maximum degradation (Emax) of 72.0%, and a DC50 value of 130.0 nM for GSPT1 degradation after 24 hours, highlighting its potential as a PROTAC agent targeting the CRBN/GSPT1 pathway..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.
别名	4 - 羟基沙利度胺, 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione

化学信息

分子量	274.23
分子式	C₁₃H₁₀N₂O₅
CAS No.	64567-60-8
Smiles	O=C1N(C(=O)C=2C1=CC(O)=CC2)C3C(=O)NC(=O)CC3
密度	1.611g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 60 mg/mL (218.79 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.29 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.6466 mL	18.2329 mL	36.4657 mL	182.3287 mL
5 mM	0.7293 mL	3.6466 mL	7.2931 mL	36.4657 mL
10 mM	0.3647 mL	1.8233 mL	3.6466 mL	18.2329 mL
20 mM	0.1823 mL	0.9116 mL	1.8233 mL	9.1164 mL
50 mM	0.0729 mL	0.3647 mL	0.7293 mL	3.6466 mL
100 mM	0.0365 mL	0.1823 mL	0.3647 mL	1.8233 mL