ND2158
Modify Date: 2024-01-13 21:15:14
ND2158 structure
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Common Name | ND2158 | ||
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| CAS Number | 1388896-07-8 | Molecular Weight | 446.566 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H30N4O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of ND2158ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199. |
| Name | ND2158 |
|---|
| Description | ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199. |
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| References | 1. Priscilla N Kelly, et al. J Exp Med. 2015 Dec 14;212(13):2189-201. 2. Giménez N, et al. Leukemia. 2020 Jan;34(1):100-114. |
| Molecular Formula | C22H30N4O4S |
|---|---|
| Molecular Weight | 446.566 |