Home Cell Cycle RUNX inhibitor - Other inhibitor XRK3F2 For research use only.

XRK3F2

XRK3F2 is an inhibitor of the p62-ZZ domain that blunts MM-induced Runx2 suppression in vitro, and induces new bone formation and remodeling in the presence of tumor in vivo.

XRK3F2 Chemical Structure

XRK3F2 Chemical Structure

CAS No. 2375193-43-2

Purity & Quality Control

Batch: S875601 DMSO]87 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.29%
99.29

XRK3F2 Related Products

Biological Activity

Description XRK3F2 is an inhibitor of the p62-ZZ domain that blunts MM-induced Runx2 suppression in vitro, and induces new bone formation and remodeling in the presence of tumor in vivo.
Targets
p62-ZZ [1]
In vitro
In vitro

XRK3F2 blocks TNFα and MM (Multiple myeloma) activation of downstream signaling from the p62-signaling hub. In addition, XRK3F2 also directly decreases osteoclast formation. It directly inhibits cell growth of primary CD138+ MM cells and human MM cell lines in vitro, without negatively affecting the growth of BMSC[1]. XRK3F2 has no effect on non-MM bearing bone. XRK3F2 blocks TNFα but not IL-1β stimulated NFκB phosphorylation in MM patient BMSC and inhibits IκBα degradation by interfering with p-IκBα activation in MM cells treated with TNFα. XRK3F2 also significantly inhibits TNFα-enhanced VCAM-1, IL-6, and RANKL expression by BMSCs from MM patients compared to vehicle. XRK3F2 directly activates caspases 3, 7, and 9 in MM cells and decreases NFκB signaling in MM results in the aggregation of caspase 8 and its downstream effector caspases. Thus, high concentrations of XRK3F2 induce apoptosis in MM cells[2].
Cell Research Cell lines MC4 cells
Concentrations 5 μM
Incubation Time 48 h
Method

MC4 cells are cultured in with or without 5TGM1 MM cells (in direct contact) for 48 h under proliferation conditions +/– XRK3F2 (5 μM). MM cells are then removed by washing and media is changed to osteogenic differentiation conditions +/– XRK3F2. MC4 cells are collected at the time of MM cell removal (day 0), and after 4 days of differentiation culture in the absence of MM cells (day 4).
In Vivo
In vivo

In vivo, XRK3F2 induces new bone formation and remodeling in the presence of tumor. The t1/2 of XRK3F2 in mice is 10.3 hours. XRK3F2 induces dramatic, local new bone formation in bones bearing MM in vivo but does not induce new bone formation in bones from the same animals that are not directly inoculated with MM cells. The results demonstrate that XRK3F2 alters the effect of MM on bone[2].
Animal Research Animal Models Specific-pathogen-free, male C57BL/KaLwRij mice (6–12 weeks of age) with implanted tumor
Dosages 27 mg/kg/day or 40 mg/kg/day
Administration i.p.

Chemical Information & Solubility

Molecular Weight 435.89 Formula

C23H24ClF2NO3
CAS No. 2375193-43-2 SDF --
Smiles Cl.OCCNCC1=CC=C(OCC2=CC=C(F)C=C2)C(=C1)OCC3=CC=C(F)C=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy XRK3F2 | XRK3F2 supplier | purchase XRK3F2 | XRK3F2 cost | XRK3F2 manufacturer | order XRK3F2 | XRK3F2 distributor