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N-(3-(2-oxo-2,3-dihydrothiazol-4-yl)-5-(thiophene-2-sulfonamido)phenyl)thiophene-2-carboxamide

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Catalog: ASIS-P017

Formal Name: N-(3-(2-oxo-2,3-dihydrothiazol-4-yl)-5-(thiophene-2-sulfonamido)phenyl)thiophene-2-carboxamide

Produced By: AsisChem, Inc.

Related Files
pdfASIS-P017 Technical Product Information (570.15 KB )
pdfASIS-P017 SDS (249.88 KB )

Biological Description

ASIS-P017, published as Compound 40a (Zhao et al. 2013), is a 2-thiazolidinone bromodomain inhibitor with high affinity for BRD3 and BRD4 (IC50 of 0.23 ± 0.04 µM, ALPHAScreen®) as well as lesser affinity for BRD2, and a short half-life of approximately 5 minutes in liver microsomes (Sharp et al. 2014). Histone modification plays a vital role in epigenetic regulation and is increasingly being studied as a mechanism and potential drug target for a variety of diseases including some carcinomas, leukemia, various inflammatory diseases and HIV. Lysine acetylation of histones is mediated by proteins containing a bromodomain, an approximately 110 amino acid conserved domain. Many of these bromodomain proteins, including BRD3, BRD4, CREBBP, TIF1?, ATAD2, and SMARCA4 are studied for their roles in disease and pathology.

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Additional Information

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Catalog ASIS-P017
Formal Name N-(3-(2-oxo-2,3-dihydrothiazol-4-yl)-5-(thiophene-2-sulfonamido)phenyl)thiophene-2-carboxamide
CAS Number 1435386-46-1
Molecular Weight 463.57
Formula C18 H13 N3 O4 S4
Lead Time 3
LogP 5.506299973
Purity 95
SMILES C1(C(NC2=CC(NS(C3SC=CC=3)(=O)=O)=CC(C3=CSC(=O)N3)=C2)=O)SC=CC=1
Solubility and Handling Room Temperature
inchikey NYMSTPKLCDJANI-UHFFFAOYSA-N
TPSA 201.2299957
HBD 3
HBA 9

Details

Bamborough, P., H. Diallo, J. D. Goodacre, L. Gordon, A. Lewis, J. T. Seal, D. M. Wilson, M. D. Woodrow and C. W. Chung (2012). "Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides." J Med Chem 55(2): 587-596. (Abstract)(Abstract)

James, L. I., D. Barsyte-Lovejoy, N. Zhong, L. Krichevsky, V. K. Korboukh, J. M. Herold, C. J. MacNevin, J. L. Norris, C. A. Sagum, W. Tempel, E. Marcon, H. Guo, C. Gao, X. P. Huang, S. Duan, A. Emili, J. F. Greenblatt, D. B. Kireev, J. Jin, W. P. Janzen, P. J. Brown, M. T. Bedford, C. H. Arrowsmith and S. V. Frye (2013). "Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain." Nat Chem Biol 9(3): 184-191. (Abstract)(Abstract)

James, L. I., V. K. Korboukh, L. Krichevsky, B. M. Baughman, J. M. Herold, J. L. Norris, J. Jin, D. B. Kireev, W. P. Janzen, C. H. Arrowsmith and S. V. Frye (2013). "Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3." J Med Chem 56(18): 7358-7371. (Abstract)(Abstract)

(Abstract)

(Abstract)

Zhao, L., D. Cao, T. Chen, Y. Wang, Z. Miao, Y. Xu, W. Chen, X. Wang, Y. Li, Z. Du, B. Xiong, J. Li, C. Xu, N. Zhang, J. He and J. Shen (2013). "Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain." J Med Chem 56(10): 3833-3851. (Abstract)(Abstract)

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Product Details

Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P017
Formal Name N-(3-(2-oxo-2,3-dihydrothiazol-4-yl)-5-(thiophene-2-sulfonamido)phenyl)thiophene-2-carboxamide
CAS Number 1435386-46-1
Molecular Weight 463.57
Formula C18 H13 N3 O4 S4
Lead Time 3
LogP 5.506299973
Purity 95
SMILES C1(C(NC2=CC(NS(C3SC=CC=3)(=O)=O)=CC(C3=CSC(=O)N3)=C2)=O)SC=CC=1
Solubility and Handling Room Temperature
inchikey NYMSTPKLCDJANI-UHFFFAOYSA-N
TPSA 201.2299957
HBD 3
HBA 9
References

Details

Bamborough, P., H. Diallo, J. D. Goodacre, L. Gordon, A. Lewis, J. T. Seal, D. M. Wilson, M. D. Woodrow and C. W. Chung (2012). "Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides." J Med Chem 55(2): 587-596. (Abstract)(Abstract)

James, L. I., D. Barsyte-Lovejoy, N. Zhong, L. Krichevsky, V. K. Korboukh, J. M. Herold, C. J. MacNevin, J. L. Norris, C. A. Sagum, W. Tempel, E. Marcon, H. Guo, C. Gao, X. P. Huang, S. Duan, A. Emili, J. F. Greenblatt, D. B. Kireev, J. Jin, W. P. Janzen, P. J. Brown, M. T. Bedford, C. H. Arrowsmith and S. V. Frye (2013). "Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain." Nat Chem Biol 9(3): 184-191. (Abstract)(Abstract)

James, L. I., V. K. Korboukh, L. Krichevsky, B. M. Baughman, J. M. Herold, J. L. Norris, J. Jin, D. B. Kireev, W. P. Janzen, C. H. Arrowsmith and S. V. Frye (2013). "Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3." J Med Chem 56(18): 7358-7371. (Abstract)(Abstract)

(Abstract)

(Abstract)

Zhao, L., D. Cao, T. Chen, Y. Wang, Z. Miao, Y. Xu, W. Chen, X. Wang, Y. Li, Z. Du, B. Xiong, J. Li, C. Xu, N. Zhang, J. He and J. Shen (2013). "Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain." J Med Chem 56(10): 3833-3851. (Abstract)(Abstract)

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