Protein degrader 1 TFA

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
50mg	$180	To Be Confirmed
100mg	$280	To Be Confirmed
250mg	$450	To Be Confirmed
500mg	$620	To Be Confirmed
1g	$950	To Be Confirmed

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Cat #: V4062 CAS #: 1631137-51-3 Purity ≥ 98%

Description: Protein degrader 1 TFA (trifluoroacetic acid salt) is a novel and potent small molecule ligand for VHL (Von Hippel-Lindau), an E3 ligase which has been targeted in many PROTACs (proteolysis-targeting chimeras). Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 ligases to a desired protein of interest. PROTACs have been successfully used to degrade numerous proteins in cells, but the peptidic E3 ligase ligands used in previous PROTACs have hindered their development into more mature chemical probes or therapeutics.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	544.59
Molecular Formula	C₂₄H₃₁F₃N₄O₅S
CAS No.	1631137-51-3
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 10 mM
	Water: N/A
	Ethanol: N/A
SMILES Code	FC(F)(F)C(O)=O.O=C([C@H](C[C@@H](O)C1)N1C([C@@H](N)C(C)(C)C)=O)NCC2=CC=C(C(SC=N3)=C3C)C=C2
Synonyms	Protein degrader 1 TFA; VH032-NH2 TFA; VHL ligand 1 TFA; Protein degrader 1 TFA , VHL-7526 TFA; VHL-7526; VHL7526; VHL 7526 trifluoroacetic acid

Related Biological Data

Schematic depiction of a bifunctional HaloPROTAC containing chloroalkane (which binds HaloTag7 fusion proteins) and a hydroxyproline derivative which binds VHL.	The average fluorescence per cell compared to vehicle control was measured by flow cytometry after 24 hour treatment with the indicated compounds and concentrations. 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. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
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.	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.	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. As expected, endogenous ERK and MEK are not degraded.ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.8362 mL	9.1812 mL	18.3624 mL	36.7249 mL
5mM	0.3672 mL	1.8362 mL	3.6725 mL	7.3450 mL
10mM	0.1836 mL	0.9181 mL	1.8362 mL	3.6725 mL
20mM	0.0918 mL	0.4591 mL	0.9181 mL	1.8362 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.