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CMPD-2

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Catalog: ASIS-P022

Formal Name: (S)-N-(3-(5-(5-(1H-indol-4-yl)-1,3,4-oxadiazol-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzyl)-2-aminopropanamide

Produced By: AsisChem, Inc.

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pdfASIS-P022 Technical Product Information (537.15 KB )

Biological Description

ASIS-P022, published as CMPD2 (Sack, Thieffine et al. 2011) is a potent pyrazole inhibitor of Co-activator Associated Arginine Methyltransferase (CARM1, also known as PRMT4) with specific affinity to CARM1 (IC50 = 0.04 µM to CARM1, >25 µM against PRMT1 and PRMT3). CARM1 influences transcription initiation, splicing, and mRNA processing through modifications of the chromatin structure (Wu, Cui et al. 2012) and is upregulated in prostate cancer (Hong, Kao et al. 2004, Majumder, Liu et al. 2006). CARM1 is responsible for the transfer of S-adenosyl methionine to arginine residues of a wide variety of proteins, including nuclear hormone receptors.

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Additional Information

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Catalog ASIS-P022
Formal Name (S)-N-(3-(5-(5-(1H-indol-4-yl)-1,3,4-oxadiazol-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzyl)-2-aminopropanamide
CAS Number None
Molecular Weight 495.46
Formula C24 H20 F3 N7 O2
Lead Time 3
LogP No
Purity 95
SMILES C([C@@H](N)C)(NCC1=CC=CC(N2C(C3=NN=C(C4C=CC=C5C=4C=CN5)O3)=CC(C(F)(F)F)=N2)=C1)=O |&1:1|
Solubility and Handling No
inchikey QGSUJFJNIKHZDK-ZDUSSCGKSA-N
TPSA No
HBD No
HBA No

Details

Hong, H., C. Kao, M. H. Jeng, J. N. Eble, M. O. Koch, T. A. Gardner, S. Zhang, L. Li, C. X. Pan, Z. Hu, G. T. MacLennan and L. Cheng (2004). "Aberrant expression of CARM1, a transcriptional coactivator of androgen receptor, in the development of prostate carcinoma and androgen-independent status." Cancer 101(1): 83-89 (Abstract).(Abstract)

Huynh, T., Z. Chen, S. Pang, J. Geng, T. Bandiera, S. Bindi, P. Vianello, F. Roletto, S. Thieffine, A. Galvani, W. Vaccaro, M. A. Poss, G. L. Trainor, M. V. Lorenzi, M. Gottardis, L. Jayaraman and A. V. Purandare (2009). "Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)." Bioorg Med Chem Lett 19(11): 2924-2927 (Abstract).(Abstract)

Majumder, S., Y. Liu, O. H. Ford, 3rd, J. L. Mohler and Y. E. Whang (2006). "Involvement of arginine methyltransferase CARM1 in androgen receptor function and prostate cancer cell viability." Prostate 66(12): 1292-1301 (Abstract).(Abstract)

Nakagawa, T. and L. Guarente (2014). "SnapShot: sirtuins, NAD, and aging." Cell Metab 20(1): 192-192 e191 (Abstract).(Abstract)

Sack, J. S., S. Thieffine, T. Bandiera, M. Fasolini, G. J. Duke, L. Jayaraman, K. F. Kish, H. E. Klei, A. V. Purandare, P. Rosettani, S. Troiani, D. Xie and J. A. Bertrand (2011). "Structural basis for CARM1 inhibition by indole and pyrazole inhibitors." Biochem J 436(2): 331-339 (Abstract).(Abstract)

Wu, J., N. Cui, R. Wang, J. Li and J. Wong (2012). "A role for CARM1-mediated histone H3 arginine methylation in protecting histone acetylation by releasing corepressors from chromatin." PLoS One 7(6): e34692 (Abstract).(Abstract)

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Product Details

Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P022
Formal Name (S)-N-(3-(5-(5-(1H-indol-4-yl)-1,3,4-oxadiazol-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzyl)-2-aminopropanamide
CAS Number None
Molecular Weight 495.46
Formula C24 H20 F3 N7 O2
Lead Time 3
LogP No
Purity 95
SMILES C([C@@H](N)C)(NCC1=CC=CC(N2C(C3=NN=C(C4C=CC=C5C=4C=CN5)O3)=CC(C(F)(F)F)=N2)=C1)=O |&1:1|
Solubility and Handling No
inchikey QGSUJFJNIKHZDK-ZDUSSCGKSA-N
TPSA No
HBD No
HBA No
References

Details

Hong, H., C. Kao, M. H. Jeng, J. N. Eble, M. O. Koch, T. A. Gardner, S. Zhang, L. Li, C. X. Pan, Z. Hu, G. T. MacLennan and L. Cheng (2004). "Aberrant expression of CARM1, a transcriptional coactivator of androgen receptor, in the development of prostate carcinoma and androgen-independent status." Cancer 101(1): 83-89 (Abstract).(Abstract)

Huynh, T., Z. Chen, S. Pang, J. Geng, T. Bandiera, S. Bindi, P. Vianello, F. Roletto, S. Thieffine, A. Galvani, W. Vaccaro, M. A. Poss, G. L. Trainor, M. V. Lorenzi, M. Gottardis, L. Jayaraman and A. V. Purandare (2009). "Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)." Bioorg Med Chem Lett 19(11): 2924-2927 (Abstract).(Abstract)

Majumder, S., Y. Liu, O. H. Ford, 3rd, J. L. Mohler and Y. E. Whang (2006). "Involvement of arginine methyltransferase CARM1 in androgen receptor function and prostate cancer cell viability." Prostate 66(12): 1292-1301 (Abstract).(Abstract)

Nakagawa, T. and L. Guarente (2014). "SnapShot: sirtuins, NAD, and aging." Cell Metab 20(1): 192-192 e191 (Abstract).(Abstract)

Sack, J. S., S. Thieffine, T. Bandiera, M. Fasolini, G. J. Duke, L. Jayaraman, K. F. Kish, H. E. Klei, A. V. Purandare, P. Rosettani, S. Troiani, D. Xie and J. A. Bertrand (2011). "Structural basis for CARM1 inhibition by indole and pyrazole inhibitors." Biochem J 436(2): 331-339 (Abstract).(Abstract)

Wu, J., N. Cui, R. Wang, J. Li and J. Wong (2012). "A role for CARM1-mediated histone H3 arginine methylation in protecting histone acetylation by releasing corepressors from chromatin." PLoS One 7(6): e34692 (Abstract).(Abstract)

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