Shopping Cart

Remove All

Your shopping cart is currently empty

Proceed to checkout Continue shopping

PROTAC HMGCR Degrader-2

Name: PROTAC HMGCR Degrader-2
Brand: TargetMol
SKU: T217122
Rating: 4.5 (1 reviews)

Catalog No. T217122 Copy Product Info

🥰Excellent

PROTACHMGCR Degrader-2 is a PROTAC degrader targeting HMGCR with an IC50 of 0.25 μM. It effectively degrades HMGCR in Insig gene-silenced human liver cancer cells (HepG2) with a DC50 of 0.12 μM. This compound's oral prodrug is PROTACHMGCR Degrader-1. By utilizing the ubiquitin-proteasome system dependent on hypoxia-inducible factor prolyl hydroxylase (VHL), PROTACHMGCR Degrader-2 reduces cholesterol levels in HepG2 cells. It is applicable in hyperlipidemia-related research.

PROTAC HMGCR Degrader-2

Copy Product Info

🥰Excellent

Catalog No. T217122

PROTAC HMGCR Degrader-2

Cas No. 2715104-46-2

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Quotation

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Resource Download

Product Introduction

Bioactivity

Description

In vitro

PROTAC HMGCR Degrader-2, also known as compound 21c, exhibits different functionalities at varying concentrations in human liver cancer cells (HepG2). At higher doses (0.01-3 μmol/L, 16 hours), it acts primarily as an HMGCR inhibitor rather than a degrader, with a maximum degradation rate (Dmax) of up to 65% at 1 μM. At 0.1 μM over 24 hours, it reduces cholesterol levels in HepG2 cells. In Insig gene-silenced HepG2 cells, PROTAC HMGCR Degrader-2 (0.01-3 μM, 0-48 hours) facilitates HMGCR degradation through a PROTAC mechanism with a DC50 of 0.12 μM and achieves a Dmax of 76% at 1 μM. When used at 1 μM for 6 hours in Insig-silenced HepG2 cells, it binds both HMGCR and VHL, leading to HMGCR degradation via the VHL-dependent ubiquitin-proteasome system.

Chemical Properties

Molecular Weight	978.3
Formula	C₅₃H₇₉N₅O₁₀S
Cas No.	2715104-46-2
Smiles	O(C(NCCCCCCCCCCC(N[C@H](C(=O)N1[C@H](C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@@H](O)C1)C(C)(C)C)=O)=O)[C@@H]4[C@]5(C(C=C[C@H](C)[C@@H]5CC[C@H](C[C@H](CC(O)=O)O)O)=C[C@H](C)C4)[H]

Storage & Solubility Information

Storage

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

Citations

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc