IC261

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IC261 (IC-261, SU-5607) 是一种有效、特异性、ATP 竞争性 CK1delta/epsilon (CK1δ/CK1ε)，IC50 为 1 uM，不会阻断 α、β 和 γ 同工型的活性。

IC261 (IC-261, SU-5607) is a potent, specific, ATP-competitive CK1delta/epsilon (CK1δ/CK1ε) with IC50 of 1 uM, does not block the activity of α, β and γ isoforms; specifically blocks phosphorylation in vivo of the CK1delta/epsilon phosphorylation sites in p53 in murine SV3T3 cells, inhibits cytokinesis causing a transient mitotic arrest; reduces pancreatic tumour cell growth in vitro and in vivo, decreases the expression levels of several anti-apoptotic proteins and sensitises cells to CD95-mediated apoptosis.(In Vitro):IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34cdc2, and p55fyn (IC50s > 100 μM). IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1?μM) increases G2/M cells after 12?h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1?μM) also induces apoptosis in the extravillous trophoblast hybrid cells. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells.(In Vivo):IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/?, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice.

IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34cdc2, and p55fyn (IC50s > 100 μM). IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1?μM) increases G2/M cells after 12?h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1?μM) also induces apoptosis in the extravillous trophoblast hybrid cells. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells.

IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/?, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice.

IC-261 | SU-5607

Metabolic Enzyme/Protease

Casein Kinase

CDK5|CK1

Cancer

——

186611-52-9

311.3319

C18H17NO4

>98% (HPLC)

DMSO: ≥ 33 mg/mL

COC1=C(/C=C2C(NC3=C/2C=CC=C3)=O)C(OC)=CC(OC)=C1

2H-Indol-2-one, 1,3-dihydro-3-[(2,4,6-trimethoxyphenyl)methylene]-

(-20℃)

With Ice Pack

≥ 2 years