7-Hydroxystaurosporine
Based on 1 publication(s) in Google Scholar
7-Hydroxystaurosporine (UCN-01), a derivative of Staurosporine (HY-15141), is a selective protein kinase C (PKC) inhibitor with antitumor activity. 7-hydroxystaurosporine induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, suppresses invasion and migration in glioblastoma cells. 7-Hydroxystaurosporine exhibits efficacy in breast cancer xenograft mouse models. 7-Hydroxystaurosporine can be used for colon carcinoma, breast cancer, glioblastoma and leukemia research.
For research use only. We do not sell to patients.
- Purity: 97.8%
- CAS No.: 112953-11-4
- Formula: C28H26N4O4
- Molecular Weight:482.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) 7-Hydroxystaurosporine
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Biological Activity
7-Hydroxystaurosporine (0-10 μM, 1 h-3 days) induces DNA fragmentation in the HL60, K562, and HT-29 cells, showing plasma membrane integrity, inducing apoptosis[1].
7-Hydroxystaurosporine (3 μM, 1-2 days) induces chromatin condensation and the formation of dense micronuclear bodies in K562 and HT29 cells[1].
7-Hydroxystaurosporine (3-10 μM, 3 h-1 day) induces cell shrinkage, membrane blebbing, chromatin condensation, and nuclear fragmentation in HL60, K562, and HT29 cells[1].
7-Hydroxystaurosporine (3-10 μM, 0-96 h) induces an early, transient activation of cyclin B1/cdc2 kinase (within 1-2 h in HL60 cells and within 24 h in HT29 cells), which precedes the onset of apoptotic DNA fragmentation and morphological changes[1].
7-Hydroxystaurosporine (24-48 h) decreases cell viability in a concentration- and time-dependent manner in U-87MG cells[2].
7-Hydroxystaurosporine (0-125 nmol/L, 24-48 h) inhibits the invasive behavior of glioblastoma U-87MG cells, which is markedly enhanced in cells expressing the tumor suppressors BRCA1 or PTEN, with increasing E-cadherin expression[2].
7-Hydroxystaurosporine (0-125 nmol/L, 48 h) inhibits cell migration in U-87MG cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL60, K562, HT29 cells
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Concentration:0-10 μM, 10 μM in HL60 cells, 3 μM in K562 and HT29 cells
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Incubation Time:1, 2, and 3 h for HL60 cells, 1, 2, and 3 days for K562 and HT29 cells
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Result:Induced apoptotic DNA fragmentation not only in HL60 but also in HT29 and K562 cells independently of p53.
Showed complete DNA fragmentation within 3 h in HL60 cells and 48 h in K562 and HT29 cells.
Showed plasma membrane integrity during apoptosis.
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Cell Line:U-87MG cells, U-87MG cells transfected with BRCA1 and PTEN
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Concentration:0, 25, 50 ,75, 100, 125 nmol/L
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Incubation Time:48 h
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Result:Markedly concentration-dependently inhibited cell invasion capacity of U-87MG cells, with reductions of approximately 12% and 25%, at 50 and 100 nmol/L, respectively.
Caused an 87% and a 90% inhibition in invasion in cells transfected with BRCA1 and PTEN, respectively.
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Cell Line:U-87MG cells
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Concentration:0, 25, 50 ,75, 100, 125 nmol/L
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Incubation Time:24 h
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Result:Increased E-cadherin levels in a concentration-dependently manner.
Resulted in approximate 2.2- and 6.3-fold increases in the E-cadherin protein at 50 and100 nmol/L, respectively.
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Cell Line:U-87MG cells
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Concentration:50 and 100 nmol/L
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Incubation Time:48 h
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Result:Showed an inhibitory effect on the migration of U-87MG cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nu/nu mice (6-7 weeks old) serially subcutaneously transplanted with Br10, MCF-7 and estrogen-independent MX-1 strains, Br-10 and MCF-7 tumor-bearing mice received estradiol and progesterone to support tumor growth[3]
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Dosage:7.5 mg/kg
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Administration:i.p., five consecutive days a week for 2 weeks
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Result:Suppressed Br-10 tumor growth with a T/C ratio of 27.0% on day 11.
Suppressed MCF-7 tumor growth with a T/C ratio of 25.0% on day 12.
Exhibited positive antitumor activity against Br-10 and MCF-7 tumor strains, but not MX-1.
Resulted in induction of p21 protein and accumulation of dephosphorylation of pRB in both Br-10 and MCF-7.
Only induced p21 in MX-1.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 112953-11-4
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Appearance Solid
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Molecular Weight 482.53
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Formula C28H26N4O4
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Color White to light yellow
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SMILES
C[C@]12N3C4=C(C5=CC=CC=C53)C([C@H](NC6=O)O)=C6C7=C4N([C@](C[C@H]([C@H]2OC)NC)([H])O1)C8=CC=CC=C78
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Synonyms
UCN-01; KRX-0601
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Solvent & Solubility
DMSO : 28 mg/mL (58.03 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (293 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Shao RG, et al 7-Hydroxystaurosporine (UCN-01) induces apoptosis in human colon carcinoma and leukemia cells independently of p53. Exp Cell Res. 1997 Aug 1;234(2):388-97. [Content Brief]
[2]. Meng QH, et al. Effect of 7-hydroxystaurosporine on glioblastoma cell invasion and migration. Acta Pharmacol Sin. 2005 Apr;26(4):492-9. [Content Brief]
[3]. Koh J, et al. UCN-01 (7-hydroxystaurosporine) inhibits the growth of human breast cancer xenografts through disruption of signal transduction. Breast Cancer. 2002;9(1):50-4. [Content Brief]
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 |
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| DMSO | 1 mM | 2.0724 mL | 10.3621 mL | 20.7241 mL | 51.8103 mL |
| 5 mM | 0.4145 mL | 2.0724 mL | 4.1448 mL | 10.3621 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0724 mL | 5.1810 mL | |
| 15 mM | 0.1382 mL | 0.6908 mL | 1.3816 mL | 3.4540 mL | |
| 20 mM | 0.1036 mL | 0.5181 mL | 1.0362 mL | 2.5905 mL | |
| 25 mM | 0.0829 mL | 0.4145 mL | 0.8290 mL | 2.0724 mL | |
| 30 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7270 mL | |
| 40 mM | 0.0518 mL | 0.2591 mL | 0.5181 mL | 1.2953 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 1.0362 mL |
7-Hydroxystaurosporine Related Classifications
HY-13661 Related Classifications
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