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CGS 27023A

CGS 27023A is a non-peptidic and orally active MMP inhibitor with the K_i values of 43, 33, 20 and 8 nM for MMP-3, MMP-1, MMP-2 amd MMP-9, respectively. CGS 27023A prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model. CGS 27023A can be used for study of arthritis.

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

CAS No.: 169799-04-6
Formula: C₁₈H₂₄ClN₃O₅S
Molecular Weight:429.92

Storage:

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

Data Sheet (270 KB)

CGS 27023A Chemical Structure

CAS No.: 169799-04-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

stromelysins 1

43 nM (Ki)

collagenases 1

33 nM (Ki)

MMP-2

20 nM (Ki)

MMP-9

8 nM (Ki)

All MMP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	6900 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]
MCF7	IC₅₀	750 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA	[PMID: 20180536]
MCF7	IC₅₀	3 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	1400 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	750 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	10 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA	[PMID: 20180536]
SK-OV-3	IC₅₀	110 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
SK-OV-3	IC₅₀	13 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]

In Vivo

CGS 27023A (oral gavage, 75 µmol/kg for 10 h) prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model^[1].

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

Chemical Information

CAS No. 169799-04-6
Molecular Weight 429.92
Formula C₁₈H₂₄ClN₃O₅S
SMILES

CC(C)[C@@H](N(S(=O)(C1=CC=C(OC)C=C1)=O)CC2=CC=CN=C2)C(NO)=O.[H]Cl
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. MacPherson LJ, et al. Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits. J Med Chem. 1997;40(16):2525-2532. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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