1. Cell Cycle/DNA Damage
  2. CDK DNA/RNA Synthesis
  3. CP681301

CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.

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CP681301 Chemical Structure

CP681301 Chemical Structure

CAS No. : 865317-32-4

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila[1].

In Vitro

CP681301 (1 µM; 96 h) shows variably cytotoxic to the tested GSC cultures but is not toxic to NHNPs[1].
CP681301 (0, 10, 50 µM; 48 h) decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs[1].
CP681301 (0, 0.5, 1 µM; ) suppresses the expression of CREB Ser133 phosphorylation[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: NHNP, N12.159, GBM121, GBM39, N08-74 cells
Concentration: 1 µM
Incubation Time: 96 h
Result: Showed variably cytotoxic to the tested GSC cultures but was not toxic to NHNPs (normal human neuro-progenitors).

Western Blot Analysis[1]

Cell Line: GBM 121, GBM39 cells
Concentration: 1 µM
Incubation Time: 48 h
Result: Suppressed the expression of CD133, OLIG2, and SOX2 and cell proliferation marker KI67.
In Vivo

CP681301 (1 mM; fed; 10 days) shows anti-tumor activity in 0- to 2-day-old adult Drosophila[1].

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

Animal Model: 0- to 2-day-old adult Drosophila (brat-RNAi tumors)[1]
Dosage: 1 mM
Administration: Fed, 10 days
Result: Reduced active phospho-dCdk5 (Y15) in tumor cells and the self-renewal properties of stem cells, increased the expression of neuronal marker ElaV in these cells and increased the median survival by 2.8-fold.
Molecular Weight

298.38

Formula

C17H22N4O

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=NNC(C2CCC2)=C1)CC3=CC=C(N(C)C)C=C3

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 : ≥ 100 mg/mL (335.14 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 3.3514 mL 16.7572 mL 33.5143 mL
5 mM 0.6703 mL 3.3514 mL 6.7029 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.18%

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 3.3514 mL 16.7572 mL 33.5143 mL 83.7858 mL
5 mM 0.6703 mL 3.3514 mL 6.7029 mL 16.7572 mL
10 mM 0.3351 mL 1.6757 mL 3.3514 mL 8.3786 mL
15 mM 0.2234 mL 1.1171 mL 2.2343 mL 5.5857 mL
20 mM 0.1676 mL 0.8379 mL 1.6757 mL 4.1893 mL
25 mM 0.1341 mL 0.6703 mL 1.3406 mL 3.3514 mL
30 mM 0.1117 mL 0.5586 mL 1.1171 mL 2.7929 mL
40 mM 0.0838 mL 0.4189 mL 0.8379 mL 2.0946 mL
50 mM 0.0670 mL 0.3351 mL 0.6703 mL 1.6757 mL
60 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3964 mL
80 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
100 mM 0.0335 mL 0.1676 mL 0.3351 mL 0.8379 mL
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CP681301 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.

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CP681301
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HY-150082
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