2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. MDM-2/p53 Apoptosis PARP
  4. NSC 146109 hydrochloride

NSC 146109 hydrochloride  (Synonyms: XI-011 hydrochloride)

Cat. No.: HY-108638 Purity: 99.89%
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NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer.

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

NSC 146109 hydrochloride

NSC 146109 hydrochloride Chemical Structure

CAS No. : 59474-01-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of NSC 146109 hydrochloride:

NSC 146109 hydrochloride Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer[1][2].

In Vitro

NSC 146109 hydrochloride (0-1 μM; 16 h) activates p53 and p21 in MCF-7 cells, and upregulates the mRNA levels of p53 target genes (p21, PUMA, BAX, PIG3)[1].
NSC 146109 hydrochloride (0.5 μM; 16 h) increases the stability of p53 protein in MCF-7 cells[1].
NSC 146109 hydrochloride (0-1 μM; 1-5 days) induces apoptosis in MCF-7 cells and triggers dose-dependent cleavage of PARP[1].
NSC 146109 hydrochloride (0-1 μM; 2-24 h) downregulates MDMX protein levels, activates p53, inhibits MDMX promoter activity, and reduces MDMX mRNA levels in MCF-7 cells[1].
NSC 146109 hydrochloride (0-1 μM; 3-4 days) reduces the viability of wild-type p53 breast cancer cells (MCF-7, ZR-75-1, ZR-75-30, MDA-MB-175VII) in a dose-dependent manner, and inhibits the viability of human cervical cancer cells HeLa, Siha and Caski, with the strongest effect on HeLa cells[1].
NSC 146109 hydrochloride (0.5-1.0 μM; 24 h) significantly inhibits long-term colony formation of human cervical cancer cell lines HeLa, Siha and Caski[2].
NSC 146109 hydrochloride (0.5-1.0 μM; 24-72 h) induces apoptosis in HeLa cells in a time- and concentration-dependent manner[2].
NSC 146109 hydrochloride (0.5-1.0 μM; 24 h) upregulates the protein levels of cleaved PARP, p53, PUMA and p21, downregulates the protein level of MDMX in HeLa, Siha and Caski cells, and enhances the stability of p53 protein in HeLa cells[2].
NSC 146109 hydrochloride (0.5-1.0 μM; 24 h) upregulates the mRNA expression of p53 target genes PUMA, p21, BAX and PIG3 in a concentration-dependent manner in HeLa cancer cells[2].
NSC 146109 hydrochloride (0.5-1.0 μM; 72 h) significantly enhances the cytotoxicity of Cisplatin (HY-17394) against human cervical cancer HeLa cells[2].
NSC 146109 hydrochloride (0.5-1.0 μM; 24 h) enhances the Cisplatin-induced upregulation of cleaved PARP and p53 expression, as well as the downregulation of MDMX expression, in human cervical cancer HeLa cells[2].
NSC 146109 hydrochloride (0.5-1.0 μM) enhances the Cisplatin-induced upregulation of mRNA expression of PUMA, p21, BAX and PIG3 in human cervical cancer HeLa cells[2].

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

NSC 146109 hydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM, 1 μM
Incubation Time: 16 h
Result: Increased cellular p53 protein levels as efficiently as known p53 activators Nutlin-3a and RITA.
Caused a dose-dependent increase in p21 protein levels.

Real Time qPCR[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM, 1.0 μM
Incubation Time: 16 h
Result: Induced dose-dependent increases in mRNA levels of the p53 target genes p21, PUMA, BAX, and PIG3, with statistically significant increases relative to DMSO control at all tested concentrations.
Achieved the greatest increase for PIG3, with a relative mRNA amount of 33.41 at 1.0 μM.

Western Blot Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.5 μM (NSC 146109 pre-incubation); 100 μg/mL (Cycloheximide (HY-12320))
Incubation Time: 16 h (NSC 146109 pre-incubation); 0-3 h (Cycloheximide)
Result: Extended the half-life of p53 protein significantly, as shown by sustained p53 levels over the 3-h Cycloheximide treatment period compared to the rapid decline in untreated control cells.

Cell Cycle Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.5 μM
Incubation Time: 24 h, 48 h, 1-5 days
Result: Increased the sub-G0/G1 (apoptotic) cell population to 18.1% after 24 hours of treatment (from 2.04% in control).
Increased the sub-G0/G1 (apoptotic) cell population to 17.7% after 48 hours of treatment (from 1.76% in control).
Caused over 40% of MCF-7 cells to be apoptotic after 5 days of treatment, compared to less than 10% in DMSO control.

Apoptosis Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.2 μM, 0.5 μM, 1.0 μM
Incubation Time: 48 h
Result: Caused a dose-dependent increase in TUNEL-positive apoptotic cells, with approximately 2% positive cells at 0.2 μM, 6% at 0.5 μM, and 7% at 1.0 μM, compared to less than 1% in DMSO control.

Western Blot Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM, 1.0 μM
Incubation Time: 2 days
Result: Induced dose-dependent cleavage of PARP, a biochemical marker of apoptosis, with increasing levels of cleaved PARP seen at higher concentrations of the compound.

Western Blot Analysis[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.1 μM, 0.25 μM, 0.5 μM, 1.0 μM (16 h incubation); 0.5 μM (time-course incubation)
Incubation Time: 16 h; 2-24 h
Result: Caused dose-dependent downregulation of MDMX protein levels, with concurrent dose-dependent upregulation of p53 and p21 protein levels.
Showed MDMX levels began decreasing 4-8 hours after treatment, coinciding with the onset of p53 activation.

Real Time qPCR[1]

Cell Line: wild-type p53 MCF-7 breast cancer cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM
Incubation Time: 16 h
Result: Caused a dose-dependent decrease in MDMX mRNA levels, with relative mRNA level reduced to approximately 0.5 at 0.5 μM, compared to 1.0 in control.

Cell Viability Assay[1]

Cell Line: wild-type p53 breast cancer cells (MCF-7, ZR-75-1, ZR-75-30, MDA-MB-175VII)
Concentration: 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1.0 μM
Incubation Time: 4 days
Result: Caused a dose-dependent decrease in cell viability in all tested cell lines.
Reduced viability to ~10% at 1.0 μM in MCF-7 cells (high MDMX expression).
Left viabilities at ~20%, ~40%, and ~20% respectively at 1.0 μM in ZR-75-1, ZR-75-30, and MDA-MB-175VII cells (low MDMX expression).

Cell Viability Assay[2]

Cell Line: HeLa, Siha, Caski human cervical cancer cells
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: 72 h
Result: Dose-dependently reduced cell viability in all three cervical cancer cell lines, with the highest proliferation inhibition observed in HeLa cells.
In Vivo

NSC 146109 hydrochloride-loaded liposome (10 mg/kg; i.p.; 3 times per week for 18 consecutive days) inhibit the growth of HeLa cell xenograft tumors in BALB/c-nude mice, with a tumor growth inhibition rate of 49.2%[2].

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

Animal Model: BALB/c-nude (female, 6-7 weeks old, subcutaneous HeLa cell xenograft)[2]
Dosage: 10 mg/kg
Administration: i.p.; three times a week; 18 days
Result: Reduced mean tumor weight to 0.41 g.
Achieved a tumor growth inhibition rate of 49.2%.
Significantly reduced tumor volume relative to control.
Caused no apparent toxicity in treated mice.
Molecular Weight

316.85

Formula

C17H17ClN2S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

[H]Cl.NC(SCC1=C2C=CC=CC2=C(C)C3=CC=CC=C13)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (263.00 mM; ultrasonic and warming and heat to 60°C; 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 3.1561 mL 15.7803 mL 31.5607 mL
5 mM 0.6312 mL 3.1561 mL 6.3121 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 (sealed storage, away from moisture). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

SDS (480 KB)

COA (250 KB) HNMR (258 KB) RP-HPLC (222 KB) MS (70 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 3.1561 mL 15.7803 mL 31.5607 mL 78.9017 mL
5 mM 0.6312 mL 3.1561 mL 6.3121 mL 15.7803 mL
10 mM 0.3156 mL 1.5780 mL 3.1561 mL 7.8902 mL
15 mM 0.2104 mL 1.0520 mL 2.1040 mL 5.2601 mL
20 mM 0.1578 mL 0.7890 mL 1.5780 mL 3.9451 mL
25 mM 0.1262 mL 0.6312 mL 1.2624 mL 3.1561 mL
30 mM 0.1052 mL 0.5260 mL 1.0520 mL 2.6301 mL
40 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9725 mL
50 mM 0.0631 mL 0.3156 mL 0.6312 mL 1.5780 mL
60 mM 0.0526 mL 0.2630 mL 0.5260 mL 1.3150 mL
80 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9863 mL
100 mM 0.0316 mL 0.1578 mL 0.3156 mL 0.7890 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:

NSC 14610959474-01-0XI-011NSC146109NSC-146109XI011XI 011MDM-2/p53ApoptosisPARPpoly ADP ribose polymerasecisplatinMDMXp53Caski human cervical cancer cellsapoptosisMCF-7 breast cancer cellsbreast cancerSiha human cervical cancer cellsHeLa human cervical cancer cellscervical cancerInhibitorinhibitorinhibit

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