2. Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. ClpP Reactive Oxygen Species (ROS) Mitochondrial Metabolism
  4. ClpP activator-2

ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity.

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

ClpP activator-2

ClpP activator-2 Chemical Structure

CAS No. : 3036751-71-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

ClpP activator-2 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity[1].

In Vitro

ClpP activator-2 potently activates purified HsClpP with an EC50 of 0.54 ± 0.12 μM[1].
ClpP activator-2 (2 h) promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 ± 0.08 μM[1].
ClpP activator-2 binds to purified HsClpP, and its dissociation constant Kd is determined as 5.01 ± 1.05 μM by ITC[1].
ClpP activator-2 (0.45 μM; 24 h) causes significant mitochondrial ultrastructural damage to AMO.1 MM cells after treatment at 0.45 μM for 24 h[1].
ClpP activator-2 (0.15-0.6 μM; 48 h) promotes the accumulation of mitochondrial reactive oxygen species (ROS) in AMO.1 and ARP1 multiple myeloma (MM) cells in a concentration-dependent manner after 48 h of treatment[1].

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

ClpP activator-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: Gradient concentrations
Incubation Time: 24 h, 48 h, 72 h
Result: Reduced cell viability in a time- and concentration-dependent manner.
For AMO.1 cells, reached IC50 values of 1.30 ± 0.08 μM (24 h), 0.68 ± 0.03 μM (48 h), and 0.08 ± 0.01 μM (72 h).
For ARP1 cells, reached IC50 values of 1.81 ± 0.14 μM (24 h), 0.86 ± 0.08 μM (48 h), and 0.21 ± 0.02 μM (72 h).

Cell Cycle Analysis[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: 0.15-0.6 μM
Incubation Time: 24 h
Result: Induced dose-dependent G1 phase.

Apoptosis Analysis[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: 0.15-0.6 μM (apoptosis assay); 0.45 μM (Western blotting)
Incubation Time: 24 h, 48 h, 72 h (apoptosis assay); 48 h (Western blotting)
Result: Induced time- and concentration-dependent apoptosis, with 95% of AMO.1 cells and 73.8% of ARP1 cells apoptotic after 72 h of 0.6 μM treatment.
Upregulated cleaved caspase-3.
Parmacokinetics
Species Dose Route Cmax T1/2 Bioavailability
Rat[1] 5 mg/kg i.v. 16733.33 ng/mL 3.854 h 38.9 %
Rat[1] 10 mg/kg p.o. 6050 ng/mL 3.198 h /
In Vivo

ClpP activator-2 (5-30 mg/kg; i.p.; once every other day; 14 days) dose-dependently inhibits the tumor growth of multiple myeloma in NOD/SCID mice[1].

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

Animal Model: NOD/SCID (female, 6-8 weeks old, subcutaneous xenograft model)[1]
Dosage: 5 mg/kg; 15 mg/kg; 30 mg/kg
Administration: i.p.; every other day; 14 days
Result: Achieved 56.7% tumor volume inhibition at 5 mg/kg.
Achieved 83.4% tumor volume inhibition at 15 mg/kg.
Achieved 91.4% tumor volume inhibition at 30 mg/kg.
Showed no treatment-related damage to major organs in the 30 mg/kg group compared to controls.
Molecular Weight

483.31

Formula

C22H19Cl2F3N4O
CAS No.
SMILES

O=C1NC(NCC2=CC=C(C(F)(F)F)C=C2)=NC3=C1CN(CC3)CC4=CC(Cl)=C(Cl)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ClpP activator-2 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

ClpP activator-23036751-71-7ClpP activator2ClpP activator 2ClpPReactive Oxygen Species (ROS)Mitochondrial MetabolismCaseinolytic protease Pcaspase-3mitochondrial respiratory chain complexes I-Vmultiple myelomaAMO.1Homo sapiens caseinolytic protease PARP1apoptosisNOD/SCID miceHsClpPmitochondrial dysfunctionInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ClpP activator-2
Cat. No.:
HY-181934
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.