2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species
  4. CADD522

CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer.

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CADD522 Chemical Structure

CADD522 Chemical Structure

CAS No. : 199735-88-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

CADD522 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CADD522

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer[1][2].

IC50 & Target[1]

RUNX2

10 nM ()

In Vitro

CADD522 (0-100 μM; 24-72 h) exhibits a strong inhibitory effect on BC cell growth and survival[1].
CADD522 (50 μM; 72 h) shows anti-proliferative effect by inducing cell cycle arrest (G1 phase)[1].
CADD522 (50 μM; 8 days) inhibits tumorsphere formation and (50 μM; 24 h) in vitro invasion of BC cells (without cellular toxicity)[1].
CADD522 (2, 10, 25, 50, 100 μM; 48 h) inhibits RUNX2 transcriptional activity by inhibiting RUNX2-DNA binding in T47D-RUNX2 and T47D-Empty cells[1].
CADD522 (50 μM; 72 h) upregulates RUNX2 levels through increased RUNX2 stability in cells[1].
CADD522 (50 μM; 6 or 24 h) increases ROS generation of mitochondrial in MCF7 and MDA-468 cells[2].
CADD522 (0-2000 nM, 30 min) inhibits mitochondrial ATP synthase activity in MDA-231 and MDA-468 cells[2].

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

CADD522 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-468, MCF7, MCF10A, IEC-6, GES-1 and C2C12 cells
Concentration: 0-100 μM
Incubation Time: 24-72 h
Result: Displayed a dose- and time-dependent cell growth inhibition over 72 h.
Exhibited low cytotoxicity for normal cell growth.

Cell Cycle Analysis[1]

Cell Line: MCF7, MDA-468 and MDA-231 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Induced MDA-231 cells accumulated at the G1 and G2/M phase whereas MCF7 and MDA-468 cells were at the G1 phase.

Cell Viability Assay[1]

Cell Line: MCF7, MCF7-tet-off cells
Concentration: 50 μM
Incubation Time: 8 days
Result: Dramatically decreased the size as well as the number of tumorspheres, and severely disrupted tumorspheres at day 4.
Showed a relatively selective effect on BC cells (did not have a significant influence on mammosphere formation of the MCF10A non-malignant mammary epithelial cells).

Cell Invasion Assay[1]

Cell Line: MCF7-tet-off (+Doxy), MCF7-tet-off (-Doxy) cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Almost abrogated the invasiveness of both MCF7-tet-off (+Doxy) and MCF7-tet-off (-Doxy) cells without cellular toxicity.

Cell Viability Assay[1]

Cell Line: T47D-RUNX2 and T47D-Empty cells
Concentration: 2, 10, 25, 50, 100 μM
Incubation Time: 48 h
Result: Resulted in a dramatic decrease of the promoter-luciferase (Luc) activities of RUNX2 downstream target genes such as MMP13 and VEGF (metastasis markers) and OC (osteogenesis marker).

RT-PCR[1]

Cell Line: T47D and MCF7 cells (ectopic expressing RUNX2)
Concentration: 50 μM
Incubation Time: 72 h
Result: Significantly inhibited the mRNA level (RUNX2-mediated) of Glut-1 and LDHA.

Western Blot Analysis[1]

Cell Line: T47D-RUNX2 and MCF7-RUNX2 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Enhanced both mRNA and protein expression of RUNX2.

Western Blot Analysis[1]

Cell Line: MDA-468 and MDA-231 cells
Concentration: 50 μM
Incubation Time: 2, 4, 6 h
Result: Increased RUNX2 stability by delaying protein degradation.

Cell Viability Assay[2]

Cell Line: MCF7 and MDA-468 cells
Concentration: 50 μM
Incubation Time: 6 or 24 h
Result: Increased the level of mitochondrial ROS, which was more evident in serum-free than serum-containing condition.

Cell Viability Assay[2]

Cell Line: MDA-231 and MDA-468 cells
Concentration: 50, 250, 2000 nM (for MDA-231); 500, 2000 nM (for MDA-468)
Incubation Time: 30 min
Result: Inhibited the activity of A TP synthase.
In Vivo

CADD522 (1, 5 and 20 mg/kg; i.p.; twice a week for 45 days) delays the onset of the tumors and suppresses tumor growth in mice[1].
CADD522 (10 mg/kg; i.p.; twice a week for 11 days) suppresses tumor metastasis and inhibits expression of Ki-67 in mice[1].

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

Animal Model: Female mice (6-week-old; MMTV-PyMT transgenic model)[1].
Dosage: 1, 5 and 20 mg/kg
Administration: Intraperitoneal injection; twice a week for 45 days.
Result: Delayed the onset of the tumors, delayed tumor development and reduced tumor burden in transgenic MMTV-PyMT mice.
Reduced the tumor weight in mice.
Animal Model: Female NOD scid gamma (NSG) mice and nude mice (TNBC-PDX Br-001 model)[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; twice a week for 11 days.
Result: Significant decreased tumor volume and markedly inhibited expression of Ki-67.
Inhibited experimental metastasis of BC cells in vivo.(did not significantly decrease body weight or influence the general health of animals).
Molecular Weight

326.17

Formula

C15H13Cl2NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(Cl)C=CC(NC(C2C(C3)C=CC3C2C(O)=O)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (766.47 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 3.0659 mL 15.3294 mL 30.6589 mL
5 mM 0.6132 mL 3.0659 mL 6.1318 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, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.17 mg/mL (6.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
  • Protocol 2

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

    Solubility: ≥ 2.17 mg/mL (6.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 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 (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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, 2 years; -20°C, 1 year (stored under nitrogen)

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
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, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0659 mL 15.3294 mL 30.6589 mL 76.6471 mL
5 mM 0.6132 mL 3.0659 mL 6.1318 mL 15.3294 mL
10 mM 0.3066 mL 1.5329 mL 3.0659 mL 7.6647 mL
15 mM 0.2044 mL 1.0220 mL 2.0439 mL 5.1098 mL
20 mM 0.1533 mL 0.7665 mL 1.5329 mL 3.8324 mL
25 mM 0.1226 mL 0.6132 mL 1.2264 mL 3.0659 mL
30 mM 0.1022 mL 0.5110 mL 1.0220 mL 2.5549 mL
40 mM 0.0766 mL 0.3832 mL 0.7665 mL 1.9162 mL
50 mM 0.0613 mL 0.3066 mL 0.6132 mL 1.5329 mL
60 mM 0.0511 mL 0.2555 mL 0.5110 mL 1.2775 mL
80 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9581 mL
100 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.7665 mL
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CADD522 Related Classifications

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.

Keywords:

CADD522199735-88-1CADD 522CADD-522Reactive Oxygen Speciesbreast cancerMCF7MDA-468MDA-231MCF7-tet-offT47D-RUNX2Inhibitorinhibitorinhibit

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