2. Autophagy
  3. p62 Autophagy
  4. XRK3F2

XRK3F2 is an inhibitor of p62 (Sequestosome-1)-ZZ/ domain.

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XRK3F2 Chemical Structure

XRK3F2 Chemical Structure

CAS No. : 2375193-43-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

XRK3F2 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

XRK3F2 is an inhibitor of p62 (Sequestosome-1)-ZZ/ domain.

IC50 & Target

P62-ZZ domain[1].
Cellular Effect
Cell Line Type Value Description References
MM1.S IC50
4.6 μM
Compound: XRK3F2
Inhibition of cell growth in human MM1.S cells incubated for 48 hrs by MTT assay
Inhibition of cell growth in human MM1.S cells incubated for 48 hrs by MTT assay
[PMID: 32193054]
In Vitro

The presence of XRK3F2 during MM-preOB co-cultures prevents Runx2 suppression at both d0 and d4. Furthermore, XRK3F2 blocks MM-induced upregulation of Gfi1. XRK3F2 blocks the induction of Gfi1 mRNA in BMSC in both treatment conditions. In contrast, XRK3F2 prevents both MM1.S CM and TNFα plus IL7-mediated Runx2 suppression. Further, the pro-inflammatory and myeloma pro-survival factor IL6 mRNA is also reduced by XRK3F2 treatment. In addition, XRK3F2 also prevents TNFα-mediated upregulation of Gfi1 and rescues inhibition of Runx2 in MC4 preOB. XRK3F2 prevents MM-induced GFI1 occupancy at the Runx2-P1 promoter. XRK3F2 treatment significantly rescues the H3K9ac levels at Runx2 in MM patient hBMSC and XRK3F2 can rescue early steps in osteogenesis[1].

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

XRK3F2 Related Antibodies
Molecular Weight

435.89

Formula

C23H24ClF2NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C=C1)=CC=C1COC2=C(OCC3=CC=C(F)C=C3)C=C(CNCCO)C=C2.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (344.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.91 mg/mL (2.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2942 mL 11.4708 mL 22.9416 mL
5 mM 0.4588 mL 2.2942 mL 4.5883 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2942 mL 11.4708 mL 22.9416 mL 57.3539 mL
DMSO 5 mM 0.4588 mL 2.2942 mL 4.5883 mL 11.4708 mL
10 mM 0.2294 mL 1.1471 mL 2.2942 mL 5.7354 mL
15 mM 0.1529 mL 0.7647 mL 1.5294 mL 3.8236 mL
20 mM 0.1147 mL 0.5735 mL 1.1471 mL 2.8677 mL
25 mM 0.0918 mL 0.4588 mL 0.9177 mL 2.2942 mL
30 mM 0.0765 mL 0.3824 mL 0.7647 mL 1.9118 mL
40 mM 0.0574 mL 0.2868 mL 0.5735 mL 1.4338 mL
50 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1471 mL
60 mM 0.0382 mL 0.1912 mL 0.3824 mL 0.9559 mL
80 mM 0.0287 mL 0.1434 mL 0.2868 mL 0.7169 mL
100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.5735 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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XRK3F2 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:

XRK3F22375193-43-2p62AutophagySequestosome-1SQSTM1Inhibitorinhibitorinhibit

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