WH23
WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C18H14O6
- Molecular Weight:326.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
WH23 (Compound WH23) potently inhibits wild-type DHRS11 with an IC50 of 0.037 ± 0.0079 μM, and its binding relies heavily on hydrogen bonding with His210 of DHRS11, as evidenced by a 24-fold loss of potency against the His210Ala mutant (IC50 = 0.87 μM)[1].
WH23 inhibit CBR1 with an IC50 of 1.7 nM and exhibits 46-fold selectivity for DHRS1[1] .
WH23 (10 μM; 2-72 h) suppresses androgen signaling and proliferation in MDA-MB-453 cells by reducing AR mRNA and protein levels, inhibiting 11KAdione (HY-135794)-induced c-Myc expression, and blocking androgen-driven cell growth[1].
WH23 (10 μM; 0.5-3 h) inhibits PI3K/AKT and MAPK signaling in MDA-MB-453 cells by reducing phosphorylation of key pathway proteins including PDK1, AKT, mTOR, and ERK[1].
WH23 (5-20 μM; 48 h) selectively reduces viability of AR-positive MDA-MB-453 triple-negative breast cancer cells, with minimal effect on AR-negative MDA-MB-231 cells[1].
WH23 (2-10 μM; 48 h) synergistically enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis in Capivasertib-resistant MDA-MB-453 cells, with combination index values less than 1 confirming synergism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-453 cells
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Concentration:10 μM
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Incubation Time:0.5, 1, or 3 h
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Result:Reduced phosphorylation of ERK (MAPK pathway), and decreased phosphorylation of PDK1, AKT, and mTOR (PI3K/AKT pathway).
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Cell Line:MDA-MB-453 (AR-positive, LAR subtype) and MDA-MB-231 (AR-negative, non-LAR subtype) triple-negative breast cancer cells
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Concentration:5, 10, 20 μM
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Incubation Time:48 h
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Result:Significantly reduced viability of MDA-MB-453 cells at concentrations of 5, 10, 15, and 20 μM, but had minimal impact on viability of MDA-MB-231 cells.
Chemical Information
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Molecular Weight 326.30
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Formula C18H14O6
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SMILES
O=C1C=C(/C=C/C2=CC=C(O)C=C2O)OC3=C(C)C(O)=CC(O)=C13
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)