PI-1840

  Cat. No.:  DC9611   Featured
Chemical Structure
1401223-22-0
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More than 5000 active chemicals with high quality for research!
Field of application
PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
Cas No.: 1401223-22-0
SMILES: O=C(N(C(C)C)CC1=NC(C2=CC=CN=C2)=NO1)COC3=CC=C(CCC)C=C3
Formula: C22H26N4O3
M.Wt: 394.4668
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
In Vivo: PI-1840 but not bortezomib suppresses the growth in nude mice of human breast tumor xenografts [1].
In Vitro: PI-1840 is over 100-fold more selective for the constitutive proteasome over the immunoproteasome. Mass spectrometry and dialysis studies demonstrate that PI-1840 is a noncovalent and rapidly reversible CT-L inhibitor. In intact cancer cells, PI-1840 inhibits CT-L activity, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis. Furthermore, PI-1840 sensitizes human cancer cells to the mdm2/p53 disruptor, nutlin, and to the pan-Bcl-2 antagonist BH3-M6 [1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC39096 MDL-28170 MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
DC8448 VR23 VR-23 is a Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E–Mediated Centrosome Amplification
DC9611 PI-1840 PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
DC8747 PD-151746 PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
DC8283 PD 150606 PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).
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