1. Epigenetics Apoptosis
  2. SF3B1 Apoptosis
  3. WX-02-23

WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer.

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

WX-02-23

WX-02-23 Chemical Structure

CAS No. : 2929223-35-6

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

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Description

WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer[1][2][3][4].

In Vitro

WX-02-23 (20 µM; 3 h) binds to FOXA1_C258 in a stereoselective and site-specific manner in 22Rv1 prostate cancer cells[1].
WX-02-23 (20 μM; 2 h) stereoselectively inhibits CJR-6A-mediated enrichment of FOXA1 in 22Rv1 prostate cancer cells (IC50 = 5.5 μM)[1].
WX-02-23 (20 µM; 3 h) remodels FOXA1 binding and chromatin accessibility in 22Rv1 prostate cancer cells[1].
WX-02-23 (200 µM; 10 min) increases the thermal stability of SF3B1 in nuclear extracts NE-3 from HeLa cells[3].
WX-02-23 (0.2–200 µM; 60 min) inhibits the splicing of precursor mRNA in HeLa cell nuclear extracts, with an IC50 of approximately 5 µM[3].
WX-02-23 (0.1-100 μM; 24-72 h) inhibits proliferation of 22Rv1 cells (IC50 = 170 nM) and induces apoptosis in THP1 cells, among others[4].

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

Cell Proliferation Assay[1]

Cell Line: Parental and C1111S-SF3B1 22Rv1 human prostate cancer cells
Concentration: 0.01-100 μM
Incubation Time: 72 h
Result: Inhibited the growth of parental 22Rv1 cells with a GI50 of 9.5 μM (95% confidence interval: 9.0-10.1 μM).
Inhibited the growth of C1111S-SF3B1 22Rv1 cells with a GI50 of 12.2 μM (95% confidence interval: 11.0-13.6 μM).

Cell Proliferation Assay[3]

Cell Line: 22Rv1 human prostate cancer cells
Concentration: dose range
Incubation Time: 72 h
Result: Exhibited minimal anti-proliferative activity, with significantly reduced potency compared to its active enantiomer WX-02-23 (IC50 not reported, as it was the inactive stereoisomer).
Molecular Weight

459.49

Formula

C26H25N3O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C=C)N([C@H](C(N1CCOCC1)=O)C2)[C@H](C3=CC=C(OCO4)C4=C3)C5=C2C6=C(N5)C=CC=C6

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 : 50 mg/mL (108.82 mM; Need ultrasonic; 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 2.1763 mL 10.8816 mL 21.7633 mL
5 mM 0.4353 mL 2.1763 mL 4.3527 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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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 2.1763 mL 10.8816 mL 21.7633 mL 54.4081 mL
5 mM 0.4353 mL 2.1763 mL 4.3527 mL 10.8816 mL
10 mM 0.2176 mL 1.0882 mL 2.1763 mL 5.4408 mL
15 mM 0.1451 mL 0.7254 mL 1.4509 mL 3.6272 mL
20 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7204 mL
25 mM 0.0871 mL 0.4353 mL 0.8705 mL 2.1763 mL
30 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8136 mL
40 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
50 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5441 mL
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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.

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Product Name:
WX-02-23
Cat. No.:
HY-168534
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