2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Androgen Receptor HSP Apoptosis
  4. Neoisoliquiritin

Neoisoliquiritin  (Synonyms: Neoisoliquiritigenin)

Cat. No.: HY-N2122 Purity: 99.74%
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Neoisoliquiritin (Neoisoliquiritigenin) is an androgen receptor (AR) inhibitor. Neoisoliquiritin inhibits the ATPase activity of GRP78. Neoisoliquiritin induces G0/G1 cell cycle arrest and inhibits proliferation in cancer cells, while it also induces cell apoptosis (apoptosis). Neoisoliquiritin suppresses tumor growth in mouse models of prostate cancer and breast cancer. Neoisoliquiritin can be used in studies related to prostate cancer and breast cancer.

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

Neoisoliquiritin

Neoisoliquiritin Chemical Structure

CAS No. : 59122-93-9

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Neoisoliquiritin Related Antibodies

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Description

Neoisoliquiritin (Neoisoliquiritigenin) is an androgen receptor (AR) inhibitor. Neoisoliquiritin inhibits the ATPase activity of GRP78. Neoisoliquiritin induces G0/G1 cell cycle arrest and inhibits proliferation in cancer cells, while it also induces cell apoptosis (apoptosis). Neoisoliquiritin suppresses tumor growth in mouse models of prostate cancer and breast cancer. Neoisoliquiritin can be used in studies related to prostate cancer and breast cancer[1][2].

Cellular Effect
Cell Line Type Value Description References
HT-22 EC50
72 μM
Compound: 21
Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay
Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay
[PMID: 32991171]
In Vitro

Neoisoliquiritin (24-72 h) potently inhibits the proliferation of human prostate cancer cell line LNCaP with an IC50 value of 19.35 μM, but exerts no effect on human prostate cancer cell line PC3[1].
Neoisoliquiritin (20-40 μM; 5 days) reduces the viability of human prostate cancer cell line LNCaP in a dose-dependent manner following 5 days of treatment[1].
Neoisoliquiritin (20-40 μM; 24-48 h) induces G0/G1 cell cycle arrest in human prostate cancer LNCaP cells by reducing the protein levels of cyclin D1 and CDK4[1].
Neoisoliquiritin (20 μM) regulates gene expression in human prostate cancer LNCaP cells, in which the androgen receptor (AR) signaling pathway serves as its key target pathway, and downregulates genes associated with cell proliferation and cell cycle progression[1].
Neoisoliquiritin (20 μM; 6-36 h) downregulates AR and its downstream target PSA at both mRNA and protein levels in LNCaP human prostate cancer cells[1].
Neoisoliquiritin (20 μM; 1-24 h) blocks DHT-induced nuclear translocation of AR in human prostate cancer LNCaP cells, and inhibits DHT-induced recruitment of AR to the androgen response element (ARE) in the PSA promoter of human prostate cancer LNCaP cells[1].
Neoisoliquiritin (10-80 μM; 24 h) inhibits the transcriptional activity of AR in AD293 cells in a dose-dependent manner (detected via PSA promoter luciferase activity), and this effect is observed after 24 h of treatment regardless of the presence or absence of DHT[1].
Neoisoliquiritigenin (20-160 μM; 48 h) inhibits the proliferation of MCF-7 and MDA-MB-231 breast cancer cells in a dose-dependent manner, reducing cell viability to approximately 10% at the highest tested concentration[2].
Neoisoliquiritigenin (20-160 μM) induces apoptosis in MCF-7 and MDA-MB-231 breast cancer cells, with a stronger effect on MDA-MB-231 cells[2].
Neoisoliquiritigenin (20-160 μM) inhibits the ATPase activity of GRP78 in a dose-dependent manner, reducing the activity to approximately 50% of that in the control group at concentrations of 80 μM and 160 μM[2].

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

Neoisoliquiritin Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP (AR-dependent human prostate cancer)
Concentration: 20, 40 μM
Incubation Time: 5 days
Result: Reduced LNCaP cell viability in a dose-dependent manner, with 20 μM and 40 μM treatments leading to significant decreases in viable cell counts relative to controls.

Cell Cycle Analysis[1]

Cell Line: LNCaP (AR-dependent human prostate cancer)
Concentration: 20, 40 μM
Incubation Time: 24 h, 48 h
Result: Increased the LNCaP cell population in the G0/G1 phase in a time-dependent manner, with concomitant decreases in S and G2/M phase populations.
Decreased cyclin D1 and CDK4 protein levels in dose- and time-dependent manners.
Did not induce statistically significant apoptosis in LNCaP cells after 24 h or 48 h of treatment.

Real Time qPCR[1]

Cell Line: LNCaP (AR-dependent human prostate cancer)
Concentration: 20 μM
Incubation Time: 6 h, 12 h, 24 h, 36 h
Result: Significantly downregulated AR mRNA levels in LNCaP cells at 24 h and 36 h, and downregulated AR protein levels relative to controls.
Significantly downregulated PSA mRNA levels at 12 h (0.5-fold), 24 h (0.3-fold), and 36 h (0.1-fold), and reduced secreted and cytoplasmic PSA protein levels relative to controls.

Immunofluorescence[1]

Cell Line: LNCaP (AR-dependent human prostate cancer)
Concentration: 20 μM (in combination with 10 nM DHT)
Incubation Time: 1 h
Result: Blocked DHT-induced nuclear accumulation of AR in LNCaP cells, where DHT treatment alone induced significant nuclear accumulation of AR, and AR was mainly localized to the cytoplasm in the absence of DHT.

Cell Proliferation Assay[2]

Cell Line: MCF-7, MDA-MB-231 breast cancer cells
Concentration: 20 μM, 40 μM, 80 μM, 160 μM
Incubation Time: 48 h
Result: Reduced MCF-7 cell survival to ~60% at 20 μM, ~40% at 40 μM, ~20% at 80 μM, and ~20% at 160 μM.
Reduced MDA-MB-231 cell survival to ~60% at 20 μM, ~40% at 40 μM, ~20% at 80 μM, and ~10% at 160 μM.
Inhibited cell survival in a dose-dependent manner with all reductions statistically significant relative to mock-treated cells.
In Vivo

Neoisoliquiritin (1 mg/kg; i.p.; every other day; for 45 consecutive days) exerts potent tumor-suppressive activity in AR-dependent prostate cancer xenograft mouse models, reduces tumor volume, AR expression levels and cell proliferation capacity, and does not induce hepatotoxicity or nephrotoxicity[1].
Neoisoliquiritigenin (25 mg/kg; i.p.; once daily; for 28 consecutive days) significantly reduces the weight of breast cancer xenografts by approximately 44.7% in MDA-MB-231 mouse models and by approximately 54.1% in MCF-7-GRP78 models[2].
Neoisoliquiritigenin (25 mg/kg; i.p.; once daily; for 8 weeks) significantly inhibits breast cancer lung metastasis by approximately 60% in the MCF-7-GRP78 mouse model, and by approximately 62.5% in the MDA-MB-231 model[2].

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

Animal Model: SCID mice (male, 4-6 weeks old, subcutaneous xenograft model via LNCaP cell injection)[1]
Dosage: 1 mg/kg
Administration: i.p.; every other day; 45 days
Result: Significantly reduced xenograft tumor volumes compared to vehicle control, with volumes lower than those in the enzalutamide group.
Significantly reduced the percentage of AR-positive cells and Ki67-positive cells in tumor tissue compared to vehicle control.
Showed no typical pathological changes in kidney and liver tissue via hematoxylin and eosin staining, indicating no nephrotoxicity or hepatotoxicity.
Animal Model: Nude mice[2]
Dosage: 25 mg/kg
Administration: i.p.; daily; 28 days
Result: Reduced mean tumor weight from ~3.8 g to ~2.1 g in MDA-MB-231 xenografts.
Reduced mean tumor weight from ~3.7 g to ~1.7 g in MCF-7-GRP78 xenografts.
Animal Model: Nude mice[2]
Dosage: 25 mg/kg
Administration: i.p.; daily; 8 weeks
Result: Reduced mean lung metastatic nodule count from ~5 to ~2 in MCF-7-GRP78 models.
Reduced mean lung metastatic nodule count from ~8 to ~3 in MDA-MB-231 models.
Molecular Weight

418.39

Formula

C21H22O9
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O)C=C1O)/C=C/C3=CC=C(O)C=C3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (159.35 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 2.3901 mL 11.9506 mL 23.9011 mL
5 mM 0.4780 mL 2.3901 mL 4.7802 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 (protect from light). 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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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 (protect from light). 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 2.3901 mL 11.9506 mL 23.9011 mL 59.7529 mL
5 mM 0.4780 mL 2.3901 mL 4.7802 mL 11.9506 mL
10 mM 0.2390 mL 1.1951 mL 2.3901 mL 5.9753 mL
15 mM 0.1593 mL 0.7967 mL 1.5934 mL 3.9835 mL
20 mM 0.1195 mL 0.5975 mL 1.1951 mL 2.9876 mL
25 mM 0.0956 mL 0.4780 mL 0.9560 mL 2.3901 mL
30 mM 0.0797 mL 0.3984 mL 0.7967 mL 1.9918 mL
40 mM 0.0598 mL 0.2988 mL 0.5975 mL 1.4938 mL
50 mM 0.0478 mL 0.2390 mL 0.4780 mL 1.1951 mL
60 mM 0.0398 mL 0.1992 mL 0.3984 mL 0.9959 mL
80 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7469 mL
100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5975 mL
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  • 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:

Neoisoliquiritin59122-93-9NeoisoliquiritigeninAndrogen ReceptorHSPApoptosisHeat shock proteinsprostate cancerMCF-7 breast cancer cellsbreast cancerβ-catenin pathwayGRP78LNCaP human prostate cancer cellsandrogen response elementPC3 human prostate cancer cellsandrogen receptorMDA-MB-231 breast cancer cellsInhibitorinhibitorinhibit

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