PROTAC Linker 4

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PROTAC Linker 4

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1799506-30-1
规格:	≥98%

包装与价格：

包装	价格(元)
50mg	电议
100mg	电议
250mg	电议
500mg	电议

产品介绍

理化性质和储存条件

	Molecular Weight: 370.87 Formula: C16H31ClO7 CAS No.: 1799506-30-1 SMILES: ClCCCCCCOCCOCCOCCOCCOCC(O)=O
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Technical Information	PROTAC Linker 4

Schematic depiction of a bifunctional HaloPROTAC containing chloroalkane (which binds HaloTag7 fusion proteins) and a hydroxyproline derivative which binds VHL. A) The enantiomers of HaloPROTACs (containing D-amino acid residues) which do not bind VHL do not induce degradation of GFP-HaloTag7, supporting the necessity of VHL binding for activity. B) Pre-treatment with excess ent-HaloPROTAC3 (1 hour) prevents degradation of GFP-HaloTag7 by HaloPROTAC3 after 24 hours. C) Pre-treatment with epoxomicin (4 hours) prevents degradation of GFP-HaloTag7 by HaloPROTAC3 after 20 hours. D)Treatment with VL285 attenuates the ability of HaloPROTAC3 to induce the degradation of GFP-HaloTag7. E) Structure of VL285. All error bars depict SEM. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.	The average fluorescence per cell compared to vehicle control was measured by flow cytometry after 24 hour treatment with the indicated compounds and concentrations. A) Comparison of HaloPROTAC3 (quintuplicate) to Hyt36 (triplicate) shows that HaloPROTAC3 is significantly more potent and efficacious. B) HaloPROTAC3 leads to 50% degradation of GFP-HaloTag7 within 4 to 8 hours. C) Significant recovery from 24 hour treatment with HaloPROTAC3 is observed after a 24 hour washout. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.	A) A study of linker length with Degradation Inducing Moiety B shows that three ethylene glycol units are optimal for the degradation of GFP-HaloTag7. B) Structures of HaloPROTACs that have weaker affinity for VHL. C) Reducing the affinity for VHL attenuates their ability to induce degradation of GFP-HaloTag7, although the effect is not necessarily linear. Immunoblotting confirms that nearly complete degradation of A) GFP-HaloTag7 is observed after 24 hour treatment with 500 nM HaloPROTAC3, with significant degradation at 50 nM HaloPROTAC3. HaloPROTAC3 can lead to degradation of other HaloTag7 fusion proteins such as B) HaloTag7-ERK1 and HaloTag7-MEK1. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

Schematic depiction of a bifunctional HaloPROTAC containing chloroalkane (which binds HaloTag7 fusion proteins) and a hydroxyproline derivative which binds VHL.

A) The enantiomers of HaloPROTACs (containing D-amino acid residues) which do not bind VHL do not induce degradation of GFP-HaloTag7, supporting the necessity of VHL binding for activity. B) Pre-treatment with excess ent-HaloPROTAC3 (1 hour) prevents degradation of GFP-HaloTag7 by HaloPROTAC3 after 24 hours. C) Pre-treatment with epoxomicin (4 hours) prevents degradation of GFP-HaloTag7 by HaloPROTAC3 after 20 hours. D)Treatment with VL285 attenuates the ability of HaloPROTAC3 to induce the degradation of GFP-HaloTag7. E) Structure of VL285. All error bars depict SEM. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

The average fluorescence per cell compared to vehicle control was measured by flow cytometry after 24 hour treatment with the indicated compounds and concentrations.

A) Comparison of HaloPROTAC3 (quintuplicate) to Hyt36 (triplicate) shows that HaloPROTAC3 is significantly more potent and efficacious. B) HaloPROTAC3 leads to 50% degradation of GFP-HaloTag7 within 4 to 8 hours. C) Significant recovery from 24 hour treatment with HaloPROTAC3 is observed after a 24 hour washout. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

A) A study of linker length with Degradation Inducing Moiety B shows that three ethylene glycol units are optimal for the degradation of GFP-HaloTag7. B) Structures of HaloPROTACs that have weaker affinity for VHL. C) Reducing the affinity for VHL attenuates their ability to induce degradation of GFP-HaloTag7, although the effect is not necessarily linear.

Immunoblotting confirms that nearly complete degradation of A) GFP-HaloTag7 is observed after 24 hour treatment with 500 nM HaloPROTAC3, with significant degradation at 50 nM HaloPROTAC3. HaloPROTAC3 can lead to degradation of other HaloTag7 fusion proteins such as B) HaloTag7-ERK1 and HaloTag7-MEK1. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.