1. Metabolic Enzyme/Protease
  2. Proteasome

Capzimin 

Cat. No.: HY-110404 Purity: 99.19%
Handling Instructions

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

For research use only. We do not sell to patients.

Capzimin Chemical Structure

Capzimin Chemical Structure

CAS No. : 2084868-04-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 623 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of Capzimin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

IC50 & Target

Target: Rpn11[1]

In Vitro

Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC50=30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI50 values of 0.67 μM and 1 μM respectively), as well as several solid tumor cell lines including NCI-H460 (non-small cell lung cancer; GI50= 0.7 μM) and MCF7 (breast cancer; GI50=1.0 μM). Immunoblotting for the processed form of caspase 3 and caspase-cleaved poly ADP-ribose polymerase in HCT116 cells confirm that Capzimin not only blocks cell growth, but also induces apoptosis[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 55.67 mg/mL (88.53 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5903 mL 7.9515 mL 15.9031 mL
5 mM 0.3181 mL 1.5903 mL 3.1806 mL
10 mM 0.1590 mL 0.7952 mL 1.5903 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Fluorescence polarization assays are performed in low-volume 384 well solid black plates in quadruplicate. The assays are performed in buffer containing 50 mM Tris-HCl pH7.5, 1mM MgCl2, 50 μM ATP, 1 mM DTT and 0.01% NP-40. The components for the assay are added in the follow sequence: 1) 5 μL compound (Capzimin, et al.) (in 3% DMSO) at different concentrations, 2) 5 μL of diluted human 26S proteasome, and 3) 5μL of substrate (3 nM Ub4- peptideOG). 100 μM Zn(cyclen)2+ is present in the titration reaction for the experiments performed with Zn(cyclen)2+. Fluorescence polarization is measured at 30°C with excitation at 480 nm and emission at 520 nm. Collected data is normalized to DMSO control and fitted to a dose-response curve to determine the IC50 value[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

HCT116 cells are treated with different concentrations of 3021 or Capzimin for 72 hours in normal or low serum medium and then mixed with CellTiter-Glo reagent to estimate cell proliferation. Measured luminescence values are normalized to DMSO control and data are fitted to a dose-response equation to determine the GI50[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

628.81

Formula

C₃₀H₂₄N₆O₂S₄

CAS No.

2084868-04-0

SMILES

O=C(C1=CC2=CC=CC(SSC3=C4N=CC(C(NCCC5=NC=CS5)=O)=CC4=CC=C3)=C2N=C1)NCCC6=NC=CS6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.19%

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Product Name:
Capzimin
Cat. No.:
HY-110404
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Capzimin

Cat. No.: HY-110404