539644

UCN-01

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

• Szinonimák: UCN-01, 7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V
• Tapasztalati képlet (Hill-képlet): C₂₈H₂₆N₄O₄
• CAS-szám: 112953-11-4
• Molekulatömeg: 482.53
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• form: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: tan; white to beige
• oldhatóság: ethanol: 1 mg/mL; DMSO: 5 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: 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
• Nemzetközi kémiai azonosító kulcs: PBCZSGKMGDDXIJ-HQCWYSJUSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

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

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable