molt-3

TJ191 is a selective anti-cancer agent, targeting low TβRIII-expressing malignant T-cell leukemia/lymphoma cells.

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.

BCL-XL-IN-3 (Compound 11) is an inhibitor of BCL-XL, with a Ki of less than 0.01 nM. It suppresses cell viability in both normal Molt-4 cells and digitonin-permeabilized Molt-4 cells, with EC50 values of 77.8 nM and 0.07 nM, respectively. BCL-XL-IN-3 can be utilized as an ADC toxin for synthesizing Clezutoclax.

Nornidulin is a depsidone originally isolated from [A. nidulans] with antibacterial activity against [M. tuberculosis] and [M. ranoe], and antifungal activity against [T. tonsurans] and [M. audouini]. It inhibits the growth of methicillin-resistant [S. aureus] (MRSA; MIC = 2 μg ml) and has larvicidal activity toward Artemia (LC50 = 1.7 μg ml). Nornidulin exhibits cytotoxic activity in MOLT-3 cells (IC50 = 35.7 μM) but not in HuCCA-1, HepG2, or A549 cells (IC50s = >116.4 μM).

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

Nidulin is a depsidone originally isolated from A. nidulans. It is active against the bacteria M. tuberculosis and M. ranoe, as well as the fungi T. tonsurans and M. audouini. It also inhibits the growth of methicillin-resistant S. aureus (MRSA; MIC = 4 μg/ml) and has larvicidal activity toward Artemia (LC50 = 2.8 μg/ml). Nidulin is cytotoxic to MOLT-3 cells (IC50 = 21.2 μM) but not HuCCA-1, HepG2, or A549 cells (IC50s = >112.7 μM). It inhibits aromatase with an IC50 value of 11.2 μM.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

6β,7β-Epoxyasteriscunolide A, a sesquiterpenoid, exhibits cytotoxicity against HL-60 and MOLT-3 leukemia cell lines, with half maximal inhibitory concentrations (IC50s) ranging from 4.1 to 5.4 μM [1].

Cyclopentenylcytosine (CPC), a nucleoside analog, effectively inhibits CTP synthetase, leading to reduced levels of cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in leukemic cells. Furthermore, it enhances the phosphorylation of 1-β-D-arabinorubosylmannosylcytidine (araC) and increases its DNA intercalation activity. In the human T lymphocyte line MOLT-3, cyclopentenylcytosine triggers apoptosis and necrosis in a dose (50-300 nM) and time (8-16 h) dependent manner. When used in conjunction with araC, cyclopentenylcytosine augments the induction of both apoptosis and necrosis, amplifying its cytotoxic effects on T lymphoblasts.

Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin that exhibits anti-inflammatory and antioxidative effects, offering protection against cardiac hypertrophy.

Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41 and a lead compound for developing novel anti-HIV-1 drugs. It scavenges DPPH free radicals with an IC50 value of 21.8 μM, inhibits aromatase activity with an IC50 value of 6.8 μM, and exhibits cytotoxic activity towards the MOLT-3 cell line with an IC50 value of 3.9 μM.