2. Cell Cycle/DNA Damage Apoptosis
  3. DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis Caspase
  4. Chromomycin A3

Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe.

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Chromomycin A3 Chemical Structure

Chromomycin A3 Chemical Structure

CAS No. : 7059-24-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Chromomycin A3:

Chromomycin A3 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Chromomycin A3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

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Description

Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe[1][2][3].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.042 μM
Compound: 1
Cytotoxicity against human A549 cells after 96 hrs by Cell Titer Glo assay
Cytotoxicity against human A549 cells after 96 hrs by Cell Titer Glo assay
[PMID: 21807523]
HCC44 IC50
0.001 μM
Compound: 1
Cytotoxicity against human HCC44 cells after 96 hrs by Cell Titer Glo assay
Cytotoxicity against human HCC44 cells after 96 hrs by Cell Titer Glo assay
[PMID: 21807523]
In Vitro

Chromomycin A3 (2.5-160 nM; 24 h, 48 h) inhibits the proliferation of cholangiocarcinoma cells KKU-213, KKU-055, and KKU-100 in a dose- and time-dependent manner, with IC50s ??of 22.48 nM, 21.14 nM, and 30.52 nM at 24 h, respectively.
Chromomycin A3 (2.5-10 nM; 24 h) induces S phase arrest of KKU-213 and KKU-055 cells at low concentrations. At high concentrations, Chromomycin A3 (10-40 nM; 24 h) induces dose-dependent apoptosis by activating the caspase-8/-9/-3 pathway, and the proportion of early and late apoptotic cells increased significantly[1].

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

Chromomycin A3 Related Antibodies

Cell Viability Assayv[1]

Cell Line: KKU-213, KKU-055, KKU-100 cholangiocarcinoma cells
Concentration: 0, 2.5, 5, 10, 20, 40, 80, 160 nM (CMA3); 0, 12.5, 25, 50, 100, 200 nM (MTA)
Incubation Time: 24 h and 48 h
Result: Reduced cell viability in a dose- and time-dependent manner, with IC50 values of 22.48±4.08 nM (KKU-213), 21.14±2.24 nM (KKU-055), and 30.52±2.91 nM (KKU-100) at 24 h; with IC50 values of 9.79±1.15 nM, 13.34±1.28 nM, and 14.74±1.34 nM at 48 h, for the respective cell lines.
In Vivo

Chromomycin A3 (0.5 mg/kg; i.v.; once per week; 3 weeks) significantly inhibits tumor growth in the Rag-2/Jak3 double-deficient mouse cholangiocarcinoma xenograft model without obvious toxicity[1].

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

Animal Model: Rag-2/Jak3 double-deficient Balb/c mouse (male; 22-25 g, 6-8 weeks old) cholangiocarcinoma xenograft model[1]
Dosage: 0.5 mg/kg
Administration: Intravenous injection via tail vein, once weekly, for 3 weeks
Result: Significantly reduced tumor growth compared to the DMSO control group, decreased tumor weight.
Resulted a significant reduction in Ki-67-positive proliferating cells, and increased expression of pro-apoptotic proteins caspase-9 and Bax in tumor tissues.
No significant toxicity was observed, as body weight and general health remained stable throughout the experiment.
Molecular Weight

1183.25

Formula

C57H82O26
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C[C@H]([C@@H]1O[C@](C[C@@H](O[C@](C[C@@H](O[C@@]3([H])C[C@](O)([C@H]([C@@H](O3)C)OC(C)=O)C)[C@@H]4O)([H])O[C@@H]4C)[C@@H]5O)([H])O[C@@H]5C)[C@@H](C([C@H]([C@@H](C)O)O)=O)OC)C=C(C=C6O[C@H]7C[C@H]([C@H]([C@H](O7)C)OC(C)=O)O[C@]8([H])C[C@H]([C@H]([C@H](O8)C)OC)O)C(C(O)=C6C)=C2O
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (84.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8451 mL 4.2256 mL 8.4513 mL
5 mM 0.1690 mL 0.8451 mL 1.6903 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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

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Concentration (final)

C2

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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: 2.5 mg/mL (2.11 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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).
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: 99.66%

SDS (643 KB)

COA (253 KB) HNMR (331 KB) LCMS (273 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. 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 0.8451 mL 4.2256 mL 8.4513 mL 21.1282 mL
5 mM 0.1690 mL 0.8451 mL 1.6903 mL 4.2256 mL
10 mM 0.0845 mL 0.4226 mL 0.8451 mL 2.1128 mL
15 mM 0.0563 mL 0.2817 mL 0.5634 mL 1.4085 mL
20 mM 0.0423 mL 0.2113 mL 0.4226 mL 1.0564 mL
25 mM 0.0338 mL 0.1690 mL 0.3381 mL 0.8451 mL
30 mM 0.0282 mL 0.1409 mL 0.2817 mL 0.7043 mL
40 mM 0.0211 mL 0.1056 mL 0.2113 mL 0.5282 mL
50 mM 0.0169 mL 0.0845 mL 0.1690 mL 0.4226 mL
60 mM 0.0141 mL 0.0704 mL 0.1409 mL 0.3521 mL
80 mM 0.0106 mL 0.0528 mL 0.1056 mL 0.2641 mL
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Chromomycin A3 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:

Chromomycin A37059-24-7Chromomycin A 3Chromomycin A-3DNA Alkylator/CrosslinkerDNA/RNA SynthesisApoptosisCaspaseInhibitorinhibitorinhibit

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