2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. ZW-1226

ZW-1226 is a dual Tyrosyl DNA phosphodiesterase 2 (TDP2) and Multidrug resistance-associated protein 1 (MRP1) inhibitor with IC50 values of 0.2 and 0.5 μM, respectively. ZW-1226 exhibits selectivity over other ABC transporters. ZW-1226 elevates intracellular GSH levels, and reverses MRP1-mediated drug resistance. ZW-1226 can be used for the research of leukemia, non-small-cell lung cancer, and multidrug resistant small-cell lung cancer.

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

ZW-1226

ZW-1226 Chemical Structure

CAS No. : 2351940-23-1

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

ZW-1226 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ZW-1226 is a dual Tyrosyl DNA phosphodiesterase 2 (TDP2) and Multidrug resistance-associated protein 1 (MRP1) inhibitor with IC50 values of 0.2 and 0.5 μM, respectively. ZW-1226 exhibits selectivity over other ABC transporters. ZW-1226 elevates intracellular GSH levels, and reverses MRP1-mediated drug resistance. ZW-1226 can be used for the research of leukemia, non-small-cell lung cancer, and multidrug resistant small-cell lung cancer[1][2].

Cellular Effect
Cell Line Type Value Description References
HeLa CC50
12 μM
Compound: 11a
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30998359]
HepG2 CC50
14 μM
Compound: 11a
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30998359]
In Vitro

ZW-1226 (1-3 nM; 72 h) significantly reduces DT40 cell viability when combined with Etoposide (HY-13629) at 3 nM[1].
ZW-1226 (0.5-50 µM; 10 min) potently inhibits MRP1 with an IC50 of 0.5 µM in Sf9 cell membrane vesicles, with selectivity indices exceeding 100 over P-gp, BCRP, MRP2, and MRP3[2].
ZW-1226 (0.5-10 µM; 30 min) inhibits MRP1-mediated calcein efflux in H69AR cells with an IC50 of 0.5 µM, and this inhibitory effect is GSH-dependent[2].
ZW-1226 (5-50 µM; 5 min) inhibits substrate-stimulated MRP1 ATPase activity in Sf9 cell membrane vesicles, with no effect on baseline ATPase activity[2].
ZW-1226 (10 µM; 72 h) fully reverses MRP1-mediated resistance to Etoposide (ETP) (HY-13629) and Doxorubicin (DOX) (HY-15142A) in H69AR cells, without exhibiting intrinsic cytotoxicity[2].
ZW-1226 (1-10 µM; 1 h) increases elevates endogenous GSH levels in H69AR cells[2].
ZW-1226 binds preferentially to the LTC4-bound conformation of bovine MRP1, interacting with key residues near the H pocket, with binding enhanced by the presence of a GSH-containing substrate[2].

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

ZW-1226 Related Antibodies

Cell Viability Assay[1]

Cell Line: DT40 chicken lymphoma cells
Concentration: 1, 3 nM
Incubation Time: 72 h
Result: decreased cell viability to 22% relative to vehicle control at 1 nM when combined with Etoposide.
Significantly decreased cell viability to less than 10% relative to vehicle control at 3 nM when combined with Etoposide.

Cell Viability Assay[2]

Cell Line: H69AR small-cell lung cancer cells, NCI-H69 cells
Concentration: 10 µM
Incubation Time: 72 h
Result: Reduced the CC50 of ETP from 161.7 µM to 2.9 µM (56-fold reduction) in H69AR cells when co-treated at 10 µM.
Reduced the CC50 of DOX from 8.7 µM to 0.2 µM (44-fold reduction) in H69AR cells when co-treated at 10 µM.
Resulted in cell viability >90% in H69AR cells when used alone at 10 µM.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC MRT Vd CL
Mice[2] 4 mg/kg i.p. 228.4 min 18.8 min 411.3 nM 38.0683 μM·min 120.9 min 79.3 L/kg 0.22 L/min/kg
Molecular Weight

420.42

Formula

C25H16N4O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N=C1C2=CC3=C(C=C(C#N)C=C3)N1C4=CC=C(OCC5=CC=CC=C5)C=C4)NC2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature, keep dry and cool

In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 4 mg/mL (9.51 mM; ultrasonic and warming and heat to 60°C; 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 2.3786 mL 11.8929 mL 23.7857 mL
5 mM 0.4757 mL 2.3786 mL 4.7571 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3786 mL 11.8929 mL 23.7857 mL 59.4643 mL
5 mM 0.4757 mL 2.3786 mL 4.7571 mL 11.8929 mL
  • 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.

ZW-1226 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:

ZW-12262351940-23-1ZW1226ZW 1226P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243TDP2CCRF-CEM cellsleukemiaMultidrug resistance-associated protein 1Tyrosyl DNA phosphodiesterase 2MRP1DT40 cellssmall-cell lung cancerH460 NSCLC cellsnon-small-cell lung cancerInhibitorinhibitorinhibit

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:
ZW-1226
Cat. No.:
HY-162753
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)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

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