2. PROTAC Apoptosis
  3. PROTACs RIP kinase
  4. PROTAC RIPK degrader-2

PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes.

For research use only. We do not sell to patients.

PROTAC RIPK degrader-2 Chemical Structure

PROTAC RIPK degrader-2 Chemical Structure

CAS No. : 1801547-16-9

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5 mg USD 450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PROTAC RIPK degrader-2 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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RIPK1 RIPK2 RIPK3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes[1][2].

IC50 & Target[1]

RIPK2

 

VHL

 

In Vitro

PROTAC RIPK degrader-2 (0-30 μM, 16 h) dose-dependently downregulates RIPK protein levels in THP-1 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC RIPK degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 0-30 μM
Incubation Time: 16 h
Result: Reduced ERRα levels by 50% and RIPK protein levels by ~20% in THP-1 cells.
Molecular Weight

1060.31

Formula

C52H65N7O11S3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(SC=N1)C2=CC=C(CNC([C@H]3N(C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOC4=CC5=C(C(NC6=CC=C(SC=N7)C7=C6)=CC=N5)C=C4S(C(C)(C)C)(=O)=O)=O)=O)C[C@H](O)C3)=O)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (141.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9431 mL 4.7156 mL 9.4312 mL
5 mM 0.1886 mL 0.9431 mL 1.8862 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 7.5 mg/mL (7.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 7.5 mg/mL (7.07 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 7.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9431 mL 4.7156 mL 9.4312 mL 23.5780 mL
5 mM 0.1886 mL 0.9431 mL 1.8862 mL 4.7156 mL
10 mM 0.0943 mL 0.4716 mL 0.9431 mL 2.3578 mL
15 mM 0.0629 mL 0.3144 mL 0.6287 mL 1.5719 mL
20 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1789 mL
25 mM 0.0377 mL 0.1886 mL 0.3772 mL 0.9431 mL
30 mM 0.0314 mL 0.1572 mL 0.3144 mL 0.7859 mL
40 mM 0.0236 mL 0.1179 mL 0.2358 mL 0.5895 mL
50 mM 0.0189 mL 0.0943 mL 0.1886 mL 0.4716 mL
60 mM 0.0157 mL 0.0786 mL 0.1572 mL 0.3930 mL
80 mM 0.0118 mL 0.0589 mL 0.1179 mL 0.2947 mL
100 mM 0.0094 mL 0.0472 mL 0.0943 mL 0.2358 mL
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PROTAC RIPK degrader-2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC RIPK degrader-21801547-16-9PROTAC RIPK degrader2PROTAC RIPK degrader 2PROTACsRIP kinaseReceptor-interacting protein kinasesRIPKPROTACPIPKDegraderAntitumorLigandInhibitorinhibitorinhibit

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