Cat. No.: HY-W072962

WX2-43

고객리뷰

Based on 1 Customer Validation

WX2-43 is a PRMT5-KLF4 inhibitor (K_d 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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.74%
CAS No.: 723754-14-1
화학식: C₁₇H₂₁ClN₂
분자량:288.82

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

WX2-43 Chemical Structure

CAS No.: 723754-14-1

사이즈

가격

재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PRMT5

11.0 nM (Kd)

Bax

All Histone Methyltransferase Isoforms :

All PAK Isoforms :

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1937	EC₅₀	0.44 μM Compound: 84; WX2-43	Anticancer activity against human HCC1937 cells assessed as cell growth inhibition Anticancer activity against human HCC1937 cells assessed as cell growth inhibition	[PMID: 33650861]
HCC38	EC₅₀	1.2 μM Compound: 84; WX2-43	Anticancer activity against human HCC38 cells assessed as cell growth inhibition Anticancer activity against human HCC38 cells assessed as cell growth inhibition	[PMID: 33650861]
MCF7	EC₅₀	0.77 μM Compound: 84; WX2-43	Anticancer activity against human MCF7 cells assessed as cell growth inhibition Anticancer activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 33650861]
MDA-MB-453	EC₅₀	2.51 μM Compound: 84; WX2-43	Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition	[PMID: 33650861]
MDA-MB-468	EC₅₀	2.5 μM Compound: 84; WX2-43	Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition	[PMID: 33650861]

In Vitro

WX2-43 (biotin-WX2-43; 0.1 nM-10 μM; 2 h) binds to PRMT5 with a K_d 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.

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.

Chemical Information

CAS No. 723754-14-1
Appearance Solid
분자량 288.82
화학식 C₁₇H₂₁ClN₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4624 mL

17.3118 mL

34.6236 mL

5 mM

0.6925 mL

3.4624 mL

6.9247 mL

10 mM

0.3462 mL

1.7312 mL

3.4624 mL

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.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhou Z, et al. A novel small-molecule antagonizes PRMT5-mediated KLF4 methylation for targeted therapy. EBioMedicine. 2019;44:98-111. [Content Brief]

[2]. Borrelli C, et al. In vivo interaction screening reveals liver-derived constraints to metastasis. Nature. 2024;632(8024):411-418. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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WX2-43

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

All Histone Methyltransferase Isoforms

All PAK Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

WX2-43

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

All Histone Methyltransferase Isoforms

All PAK Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

WX2-43 Related Classifications

HY-W072962 Related Classifications