2. Epigenetics Cytoskeleton Cell Cycle/DNA Damage Apoptosis MAPK/ERK Pathway
  3. Histone Methyltransferase PAK Bcl-2 Family KLF
  4. WX2-43

WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.

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

WX2-43

WX2-43 Chemical Structure

CAS No. : 723754-14-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

WX2-43 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All PAK Isoform Specific Products:

View All Isoforms
PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

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Description

WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer[1][2].

IC50 & Target[1]

PRMT5

11.0 nM (Kd)

Bax

 

In Vitro

WX2-43 (biotin-WX2-43; 0.1 nM-10 μM; 2 h) binds to PRMT5 with a Kd of 11.0 nM[1].
WX2-43 (0.03-10 μM; 24 h) inhibits cell viability in a KLF4-dependent manner in MEFs treated with cisplatin[1].
WX2-43 is more potent in TNBC cell lines (EC50 0.44-0.96 μM) than in normal mammary epithelial cell lines (EC50 3.62-23.34 μM)[1].
WX2-43 can induce a mesenchymal-like phenotype in two-dimensional (2D) AKPS cultures, altering colony morphology, size, and actin cytoskeleton, and reducing the frequency of Ki-67+ cells[2].

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

WX2-43 Related Antibodies

Cell Viability Assay[1]

Cell Line: KLF4+/+ MEFs, KLF4-/- MEFs
Concentration: 0, 0.03, 0.1, 0.3, 1, 3, 10 μM (WX2-43); 5 μM (cisplatin)
Incubation Time: 24 h
Result: Reduced viability in KLF4+/+ MEFs in a dose-dependent manner; showed no effect on viability in KLF4-/- MEFs.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Decreased KLF4 protein levels and p21 levels and increased Bax levels in a dose-dependent manner.
In Vivo

WX2-43 (40-80 mg/kg; i.p.; twice weekly; 4 weeks) suppresses triple negative breast tumor progression in nude mice[1].

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

Animal Model: Crl: Nu-Foxn1(nu) (female, 8 weeks old)[1]
Dosage: 40 mg/kg; 80 mg/kg
Administration: i.p.; twice weekly; 4 weeks
Result: Reduced tumor size and weight by approximately 40% at 40 mg/kg compared to vehicle; Reduced tumor size and weight by approximately 60% at 80 mg/kg compared to vehicle; Confirmed reduced KLF4 protein levels in treated groups via western blotting.
Molecular Weight

288.82

Formula

C17H21ClN2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C=C1)NCC2=CC=C(C=C2)N(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (346.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4624 mL 17.3118 mL 34.6236 mL
5 mM 0.6925 mL 3.4624 mL 6.9247 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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, 6 months; -20°C, 1 month. 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
DMSO 1 mM 3.4624 mL 17.3118 mL 34.6236 mL 86.5591 mL
5 mM 0.6925 mL 3.4624 mL 6.9247 mL 17.3118 mL
10 mM 0.3462 mL 1.7312 mL 3.4624 mL 8.6559 mL
15 mM 0.2308 mL 1.1541 mL 2.3082 mL 5.7706 mL
20 mM 0.1731 mL 0.8656 mL 1.7312 mL 4.3280 mL
25 mM 0.1385 mL 0.6925 mL 1.3849 mL 3.4624 mL
30 mM 0.1154 mL 0.5771 mL 1.1541 mL 2.8853 mL
40 mM 0.0866 mL 0.4328 mL 0.8656 mL 2.1640 mL
50 mM 0.0692 mL 0.3462 mL 0.6925 mL 1.7312 mL
60 mM 0.0577 mL 0.2885 mL 0.5771 mL 1.4427 mL
80 mM 0.0433 mL 0.2164 mL 0.4328 mL 1.0820 mL
100 mM 0.0346 mL 0.1731 mL 0.3462 mL 0.8656 mL
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WX2-43 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:

WX2-43723754-14-1Histone MethyltransferasePAKBcl-2 FamilyKLFp21 activated kinasesKrüppel-like factorcolorectal cancertriple negative breast cancerKi-67AKPS colorectal cancer organoidsnude miceKLF4MDA-MB-231 cellsZEB1PRMT5MEFsInhibitorinhibitorinhibit

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