2. Epigenetics TGF-beta/Smad Cell Cycle/DNA Damage Apoptosis Cytoskeleton
  3. PKC CDK Apoptosis Cadherin
  4. 7-Hydroxystaurosporine

7-Hydroxystaurosporine  (Synonyms: UCN-01; KRX-0601)

Cat. No.: HY-13661 Purity: 97.8%
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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.

7-Hydroxystaurosporine

7-Hydroxystaurosporine Chemical Structure

CAS No. : 112953-11-4

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Based on 1 publication(s) in Google Scholar

7-Hydroxystaurosporine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 7-Hydroxystaurosporine

View All PKC Isoform Specific Products:

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

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[1][2][3].

In Vitro

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.

7-Hydroxystaurosporine Related Antibodies

Apoptosis Analysis[1]

Cell Line: HL60, K562, HT29 cells
Concentration: 0-10 μM, 10 μM in HL60 cells, 3 μM in K562 and HT29 cells
Incubation Time: 1, 2, and 3 h for HL60 cells, 1, 2, and 3 days for K562 and HT29 cells
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.

Cell Invasion Assay[2]

Cell Line: U-87MG cells, U-87MG cells transfected with BRCA1 and PTEN
Concentration: 0, 25, 50 ,75, 100, 125 nmol/L
Incubation Time: 48 h
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.

Western Blot Analysis[2]

Cell Line: U-87MG cells
Concentration: 0, 25, 50 ,75, 100, 125 nmol/L
Incubation Time: 24 h
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.

Cell Migration Assay [2]

Cell Line: U-87MG cells
Concentration: 50 and 100 nmol/L
Incubation Time: 48 h
Result: Showed an inhibitory effect on the migration of U-87MG cells.
In Vivo

7-Hydroxystaurosporine (7.5 mg/kg, i.p., five consecutive days a week for 2 weeks) exhibits antitumor effect in Br-10 and MCF-7 breast cancer xenograft mouse models[3].

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

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]
Dosage: 7.5 mg/kg
Administration: i.p., five consecutive days a week for 2 weeks
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.
Clinical Trial
Molecular Weight

482.53

Formula

C28H26N4O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0724 mL 10.3621 mL 20.7241 mL
5 mM 0.4145 mL 2.0724 mL 4.1448 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 97.8%

SDS (396 KB)

COA (269 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 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
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7-Hydroxystaurosporine 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:

7-Hydroxystaurosporine112953-11-4UCN-01 KRX-0601UCN01UCN 01KRX0601KRX 0601KRX-0601PKCCDKApoptosisCadherinProtein kinase CCyclin dependent kinaseStaurosporinebreast cancer xenograft mouse modelsHL60K562HT-29U-87MGInhibitorinhibitorinhibit

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