HIV-1 inhibitor-43

Names

[ CAS No. ]:
2493426-43-8

[ Name ]:
HIV-1 inhibitor-43

Biological Activity

[Description]:

HIV-1 inhibitor-43 (compound 12) is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection

[Target]

HIV-1 (Y188L):21.3 nM (EC50)

HIV-1 (K103N+Y181C):6.2 nM (EC50)

HIV-1 (K103N):<0.7 nM (EC50)

HIV-1 (Y181C):<0.7 nM (EC50)


[In Vitro]

HIV-1 inhibitor-43 (compound 12) has anti-HIV-1 activity against HIV-1 reverse transcriptase with IC50s of 83±8 nM, 73±8 nM, 61±6 nM and 76±8 nM for HIV-1 WT, K103N, Y181I and K103N-Y181I, respectively[1]. HIV-1 inhibitor-43 (1, 5 and 25 nM) causes 100% reduction of HIV-1 RNA and protein p24 at 25 nM in C8166 cells infected with a WT strain[1].

[References]

[1]. Nalli M, et al. New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. Eur J Med Chem. 2020 Dec 15;208:112696.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H21ClN2O4S

[ Molecular Weight ]:
468.95

Related Compounds