539644

UCN-01

A cell-permeable Staurosporine derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases.

• 別名: UCN-01, 7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V
• 実験式（ヒル表記法）: C₂₈H₂₆N₄O₄
• CAS番号: 112953-11-4
• 分子量: 482.53
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: tan; white to beige
• 溶解性: ethanol: 1 mg/mL; DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• InChI: 1S/C28H26N4O4/c1-28-25(35-3)15(29-2)12-18(36-28)31-16-10-6-4-8-13(16)19-21-22(27(34)30-26(21)33)20-14-9-5-7-11-17(14)32(28)24(20)23(19)31/h4-11,15,18,25,27,29,34H,12H2,1-3H3,(H,30,33)/t15-,18-,25-,27-,28+/m1/s1
• InChI Key: PBCZSGKMGDDXIJ-HQCWYSJUSA-N

詳細

詳細

A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC₅₀ = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC₅₀ = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC₅₀ = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents.

生物化学的／生理学的作用

Cell permeable: yes

IC50 = 29 nM, 34 nM, 30 nM, 590 nM, 530 nM, 7 nM, 27 nM, 50 nM, 50 nM, 150 nM, 1.04 µM, 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 µM, respectively for primary targets in the order listed

Primary Target
PKCα, PKCβ, PKCγ, PKCδ PKCε, Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2, PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA

Product competes with ATP.

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Reinhardt, H.C., et al. 2007. Cancer Cell11, 175.
Jiang, X., et al. 2004. Mol. Cancer Ther.3, 1221.
Sato, S., et al. 2002. Oncogene21, 1727.
Patel, V., et al. 2002. Clin. Cancer Res.8, 3549.
Leclerc, S., et al. 2001. J. Biol. Chem.276, 251.
Busby, E.C., et al. 2000. Cancer Res.60, 2108.
Hsueh, C.T., et al. 1998. Clin. Cancer Res.4, 2201.
Akiyama, T., et al. 1997. Cancer Res.57, 1495.
Seynaeve, C.M., et al. 1994. Mol. Pharmacol.45, 1207.
Takahashi, I., et al. 1987, J. Antibiot.40, 1782.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable