| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
| Targets |
CM10 targets the aldehyde dehydrogenase 1A (ALDH1A) family of enzymes, which includes ALDH1A1, ALDH1A2, and ALDH1A3. These enzymes are responsible for the oxidation of aldehydes to their corresponding carboxylic acids, utilizing NAD(P)+ as a cofactor. ALDH1A enzymes play crucial roles in numerous physiological and pathological processes, including retinoic acid biosynthesis, detoxification of reactive aldehydes, and the maintenance of stem cell populations. Overexpression of ALDH1A enzymes, particularly ALDH1A1 and ALDH1A3, has been associated with cancer stem cell phenotypes, chemotherapy resistance, and poor prognosis in various malignancies, making them attractive targets for anticancer therapy.
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| ln Vitro |
CM10 (12.5, 25, 50, and 100 μM; 1 hour) selectively kills CD133+ late-stage cancer stem-like cells (CSC) and suppresses ALDEFLUOR activity in living cells [1]. Tumor flow pattern in cells and nuclei is induced by CM10 [1].
In vitro, CM10 has been shown to inhibit ALDH1A enzyme activity, reducing the ALDH-bright (ALDHbr) population of cancer stem cells. By inhibiting ALDH1A, CM10 may sensitize cancer cells to chemotherapy and radiotherapy, as ALDH1A enzymes contribute to the detoxification of reactive aldehydes and the maintenance of stem cell properties. In cell-based assays, CM10 has been demonstrated to reduce the proliferation and clonogenic potential of cancer cell lines with high ALDH1A expression. The peptide's mechanism of action involves the direct inhibition of ALDH1A enzymatic activity, leading to the accumulation of toxic aldehydes and the disruption of retinoic acid signaling. |
| ln Vivo |
In vivo, CM10 has the potential to demonstrate antitumor efficacy by targeting ALDH1A-expressing cancer stem cells. By inhibiting ALDH1A activity, CM10 may reduce the tumor-initiating capacity of cancer stem cells and enhance the efficacy of conventional chemotherapeutic agents. The peptide's ability to target the ALDH1A family makes it a promising candidate for combination therapy approaches aimed at overcoming drug resistance and preventing tumor recurrence. However, the in vivo efficacy of CM10 has not been extensively reported, and further studies are needed to characterize its antitumor activity and pharmacokinetic properties.
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| Enzyme Assay |
In vitro enzyme assays for CM10 involve measuring its inhibition of ALDH1A enzymatic activity. The assay is typically performed using recombinant ALDH1A enzymes and a fluorogenic or colorimetric substrate, such as Aldehyde Dehydrogenase Substrate (ALDH substrate) in the presence of NAD(P)+. The enzyme is incubated with the substrate and varying concentrations of CM10, and the formation of the product is measured spectrophotometrically or fluorometrically. The IC₅₀ value is calculated from the concentration-response curve to determine the compound's potency against ALDH1A isoforms.
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| Cell Assay |
In vitro cellular experiments for CM10 are performed using cancer cell lines with high ALDH1A expression, such as breast, lung, or ovarian cancer cells. Cells are treated with varying concentrations of CM10, and the ALDHbr population is assessed using the ALDEFLUOR assay, a flow cytometry-based method that measures ALDH enzymatic activity. The effects of CM10 on cell proliferation, clonogenic potential, and chemosensitivity are assessed using standard cell-based assays. The expression of ALDH1A and stem cell markers is measured by qPCR or Western blot.
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| Animal Protocol |
In vivo animal studies for CM10 are conducted using immunocompromised mice bearing subcutaneous human tumor xenografts with high ALDH1A expression. Tumor-bearing mice are randomized into treatment and control groups and administered CM10 via intraperitoneal or subcutaneous injection at various doses. Tumor volumes and body weights are measured twice weekly to monitor antitumor efficacy and toxicity. At the end of the study, tumors are collected for histopathological analysis and to measure ALDH1A activity and stem cell marker expression.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of CM10 have not been extensively characterized in the literature. As a peptide, CM10 is expected to have a short half-life in circulation due to rapid proteolytic degradation and renal clearance. The peptide's bioavailability following subcutaneous or oral administration is likely to be limited. Various formulation strategies, such as PEGylation or encapsulation in nanoparticles, may be explored to improve its pharmacokinetic properties and prolong its duration of action for potential therapeutic applications.
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| Toxicity/Toxicokinetics |
The toxicity profile of CM10 has not been extensively characterized in the literature. As a peptide targeting ALDH1A enzymes, it is expected to have a targeted mechanism of action with limited off-target effects. However, ALDH1A enzymes play important roles in normal physiology, including retinoic acid biosynthesis and detoxification, and their inhibition may lead to on-target toxicities. Standard toxicology studies would be required to fully characterize its safety profile and therapeutic window.
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| References | |
| Additional Infomation |
CM10 is a synthetic peptide inhibitor of the ALDH1A family of enzymes, derived from the C-terminal region of CXCL10. It represents a valuable research tool for studying the role of ALDH1A enzymes in cancer stem cell biology, drug resistance, and metabolic regulation. By inhibiting ALDH1A activity, CM10 has the potential to sensitize cancer cells to chemotherapy and radiotherapy, making it a promising candidate for combination therapy approaches. Further studies are needed to fully characterize its in vivo efficacy, pharmacokinetic properties, and safety profile.
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| Molecular Formula |
C20H23N3O
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|---|---|
| Molecular Weight |
321.416124582291
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| Exact Mass |
321.184
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| CAS # |
692269-09-3
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| PubChem CID |
889692
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| Appearance |
Light green to green solid powder
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| Density |
1.12±0.1 g/cm3(Predicted)
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| Boiling Point |
512.4±52.0 °C(Predicted)
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
24
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| Complexity |
402
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C2=CC=CC=C2N=C1NCC3=CC=CC(=C3O)CC=C
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| InChi Key |
ZFHWEWJDCFGRBO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H23N3O/c1-3-8-15-9-7-10-16(19(15)24)14-21-20-22-17-11-5-6-12-18(17)23(20)13-4-2/h3,5-7,9-12,24H,1,4,8,13-14H2,2H3,(H,21,22)
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| Chemical Name |
2-prop-2-enyl-6-[[(1-propylbenzimidazol-2-yl)amino]methyl]phenol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~388.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1112 mL | 15.5560 mL | 31.1119 mL | |
| 5 mM | 0.6222 mL | 3.1112 mL | 6.2224 mL | |
| 10 mM | 0.3111 mL | 1.5556 mL | 3.1112 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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