k-103

GSK-1034702 is an M1 mAChR agonist that improves cognitive deficits and may be useful in the study of neurologic disorders.

OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.

GSK-1034702 HCl is a potent M1 receptor allosteric agonist.

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

K103 Hydrochloride, an inhibitor of peptidoglycan synthesis, targets the lipid II precursor.

BMS-561390, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

N-Desmethyl Sildenafil is the major metabolite of Sildenafil, a potent phosphodiesterase type 5 (PDE5) inhibitor.

Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV/AIDS.

HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 50 nM against the mutant E138K strain and 20.8 nM against HIV-1 WT. HIV-1 inhibitor-41 exhibits low hERG inhibition, no apparent CYP enzymatic inhibition, and no acute toxicity [1].

HIV-1 inhibitor-15 (compound 9d) is a potent, broad-spectrum inhibitor targeting HIV-1, with EC50 values of 1.7 nM against HIV-1 WT, 4 nM against L100I, 2 nM against K103N, 6 nM against Y181C, and 9 nM against E138K. It exhibits high efficacy, favorable solubility, safety profiles, and oral bioavailability [1].

HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1, and exhibits inhibitory activity against HIV-1 K103N, E138K, Y181C, and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM, and 35 nM, respectively. It demonstrates good solubility, hepatic microsomal stability, and lacks significant CYP enzyme inhibitory activity or acute toxicity.

HIV-1 inhibitor-42 (compound 5b) is a potent inhibitor of HIV-1 with an IC50 of 0.06 μM. It inhibits HIV-1 RT RNA-dependent DNA polymerase with an IC50 of 0.518 μM and DNA-dependent DNA polymerase with an IC50 of 0.072 μM.

HIV-1 inhibitor-25 (compound R-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) with an IC50 of 0.1061 nM. It exhibits a high antiviral effect against wild-type HIV-1 (EC50: 13.6 nM) and demonstrates low cytotoxicity (to MT). It also inhibits HIV-1 mutants (L100I, K103 N, Y181C, Y188L, E138K, F227L+V106A) with EC50 values ranging from 0.1961 to 5.8136 μM. HIV-1 inhibitor-25 is useful for studying AIDS.

HIV-1 inhibitor-40 (Compound 4ab), an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) with an EC50 of 1.9 nM, exhibits no significant acute toxicity in vivo and functions as a highly sensitive inhibitor of the orexin receptor antagonist CYP.

HIV-1 inhibitor-43 is a potent inhibitor of HIV-1, acting on HIV-1 Y188L (EC50: 21.3 nM), K103N-Y181C (EC50: 6.2 nM), K103N (EC50 < 0.7 nM), and Y181C (EC50 < 0.7 nM). HIV-1 inhibitor-43 reduces the expression of HIV-1 RNA and protein p24.

HIV-1 inhibitor-21 (compound 9b) is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) with an IC50 of 0.55 μM. It inhibits both wild-type HIV-1 (EC50: 12.7 nM) and mutant virus strain K103N (EC50: 10.4 nM), demonstrating relatively low cytotoxicity (CC50 for MT-4: 10.2 μM).

HIV-1 inhibitor-22 is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) (HIV-1 RT: IC50=3.63 μM). M and also showed low cytotoxicity with a CC50 > 227 μM.

HIV-1 inhibitor-14 is a potent, broad-spectrum inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) (IC50=0.14 μM for HIV-1 RT). HIV-1 inhibitor-14 inhibits both wild-type and drug-resistant HIV-1 strains (EC50: 5.79-28.3 nM).

HIV-1 inhibitor-23 is a highly potent inhibitor of HIV-1 non-nucleoside reverse transcriptase, acting on both wild-type HIV-1 (EC50: 24.9 nM) and mutant strain K103N (EC50: 10.4 nM). microsomal stability in vitro.

HIV-IN-5 (compound 5r) is a potent inhibitor of HIV-1 with an IC50 of 0.16 μM, binding to NNIBP [NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding sites].

ZLM-66 is a doravirine analogue and a potent inhibitor of non-nucleoside reverse transcriptases (NNRTIs), acting on wild-type HIV-1 reverse transcriptase (IC50: 41 nM), wild-type HIV-1 (EC50: 13 nM) and cIAP1 (EC50: 0.32 nM). ZLM-66 can be used in AIDS research.

GSK1030058A is a novel inhibitor of polo-like kinase

GKK1032B is a fungal metabolite that has antiproliferative and antibacterial activities. GKK1032B inhibits the growth of HeLa S3 cervical and MCF-7 breast cancer cells and Vero cells. It also inhibits the growth of B. subtilis and M. tuberculosis.

Reverse transcriptase-IN-3, a pyrimidine-5-carboxamide derivative, functions as an inhibitor of HIV-1, demonstrating potent activity against both wild-type and mutant strains of HIV-1.