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Background: According to preliminary results from studies treating prostate cancer cells, SGI-1776 dose-dependently reduces phosphorylation of known Pim kinase substrates involved in cell cycle progression and apotosis (p21Cip1/WAF1 and Bad), compromises overall cell viability by inducing G1 cell cycle arrest and triggering apoptosis, and reduces cell viability in a multidrug resistance 1 (MDR1) protein based taxane-refractory prostate cancer cell line.
Biological Activity: SGI-1776 inhibits Pim1, Pim2, Pim3, and FLT3 with IC50 values of 7 nM, 363 nM, 69 nM, and 44nM respectively.
CAS Number: 1025065-69-3
Description: SGI-1776 is a potent ATP-competitive inhibitor of the serine/threonine family of Pim kinase, an enzyme regulating cell survival. Through extensive biomedical characterization, SGI-1776 exhibits specificity to the three isoforms of the Pim family, including Pim-1, Pim-2, and Pim-3. Treatment with SGI-1776 induces apoptosis in CLL primary cell line.
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Pim1
Biosafety Level: Not applicable (BSL-1)
References: 1. Mumenthaler, SM., et al. Mol Cancer Ther. 2009; 8(10): 2882-2893.
2. Lisa S. Chen, LS et al. Blood. 2009; 114(19): 4150-4157.
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