1388896-07-8

1388896-07-8 structure

Name: ND2158
Chemical Name: ND2158
CAS Number: 1388896-07-8
Molecular Formula: C₂₂H₃₀N₄O₄S
Molecular Weight: 446.566
Catalog: Signaling Pathways Immunology/Inflammation IRAK
Create Date: 2022-07-01 19:36:43
Modify Date: 2024-01-13 21:15:14
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.

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.
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