UCN-01 Property

Boiling point:

705.7±60.0 °C(Predicted)

Density 

1.63±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: >5mg/mL

form 

Tan solid

pka

12.25±0.70(Predicted)

color 

light yellow

optical activity

[α]20/D 130 to 160°, c = 0.2 in DMSO

Safety

WGK Germany 

3

RTECS 

KC6600010

Toxicity

mouse,LD50,intraperitoneal,25mg/kg (25mg/kg),Journal of Antibiotics. Vol. 42, Pg. 571, 1989.

Hazard and Precautionary Statements (GHS)

UCN-01 Chemical Properties,Usage,Production

Description

UCN-01 is a synthetic derivative of staurosporine with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC₅₀ = 30 nM), PDK1 (IC₅₀ = 6 nM) and cyclin-dependent kinases (IC₅₀s = 300-600 nM for Cdk1 and Cdk2). UCN-01 arrests tumor cells in the G₁/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G₂ checkpoint kinase Chk1 (IC₅₀ = 7 nM), leading to apoptosis.

Uses

UCN-01 is an indolocarbazole isolated from a high staurosporine-producing Streptomyces culture. UCN-01 inhibits protein kinase C (PKC) and cyclin-dependant kinase 2 (CDK2), resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by the latter agents.

Uses

UCN 01 is a protein kinase C inhibitor which overrides ZEB1-induced chemoresistance in hepatocellular cancer in human. A cell-permeable Staurosporine derived anticancer agent that inhibits several protein kinases.

General Description

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.

Biochem/physiol Actions

Cell permeable: yes