1. Metabolic Enzyme/Protease Apoptosis
  2. Carbonic Anhydrase Apoptosis
  3. hCAIX/XII-IN-5

hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis.

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hCAIX/XII-IN-5 Chemical Structure

hCAIX/XII-IN-5 Chemical Structure

CAS No. : 2421127-99-1

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Description

hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis[1].

IC50 & Target

hCA XII

85.7 nM (Ki)

hCA IX

93.9 nM (Ki)

In Vitro

hCAIX/XII-IN-5 (2.36-32.17 μM) treatment shows both anti-proliferative activities to MCF-7 and PANC-1 cells under the normoxic and hypoxic condition[1].
hCAIX/XII-IN-5 (2.69 μM; 24 h) treatment shows accumulation of MCF-7 cells in the Sub-G1 phase and cell arrest in G2-M phase[1].
hCAIX/XII-IN-5 (2.69 μM; 24 h) treatment increases the percent of annexin V-FITC-positive apoptotic cells, including both the early and late apoptotic cells (UR+LR) [1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7 and PANC-1 cells
Concentration: 2.36-32.17 μM
Incubation Time:
Result: Exerted anti-proliferative activities to MCF-7 and PANC-1 cells (IC50=2.69 μM and 32.17 μM, respectively) under the normoxic condition, and moderate activitits against both MCF-7 and PANC-1 cells (IC50=16.36 μM and 11.78 μM, respectively) under the hypoxic condition.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2.69 μM
Incubation Time: 24 hours
Result: Resulted in a significant increase in the percentage of cells at Sub-G1 by 14-folds with significant increase in cell percentage in the G1-M phase by 2.3-folds compared to the control.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2.69 μM
Incubation Time: 24 hours
Result: Resulted in a significant increase in the percent of annexin V-FITC-positive apoptotic cells, including both the early (from 0.61% to 6.77%) and late apoptotic (from 0.27% to 14.84%) cells (UR+LR), about 11- and 55-fold increase, respectively, as compared with the control.
Molecular Weight

291.30

Formula

C18H13NO3

CAS No.
SMILES

O=C1C(C(/C=C/NC2=CC=CC=C2)=O)=CC3=C(O1)C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
hCAIX/XII-IN-5
Cat. No.:
HY-150695
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