Activators & Inhibitors

Veratric acid (Legacy Tebubio ref. 282T3744). Veratric acid (3,4-Dimethoxybenzoic acid) is a benzoic acid derivative from plants and fruits, possessing antioxidant, anti-inflammatory, and blood pressure-lowering properties.

C2 Adamantanyl Galactosylceramide (d18:1/2:0) (Legacy Tebubio ref. 282T37440). C2 Adamantanyl Galactosylceramide (d18:1/2:0) (AdaGalCer) is a bioactive sphingolipid. It reduces globotriaosylceramide 3 synthesis from exogenous lactosylceramide in microsomes. AdaGalCer stimulates recombinant glucocerebrosidase activity in a pH-dependent manner. It activates glucocerebrosidase to decrease glucosylceramide accumulation in fibroblasts and lymphoblasts isolated from patients with Gaucher and Fabry disease, respectively.

KMN-80 (Legacy Tebubio ref. 282T37441). The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerabi

Aspergillin PZ (Legacy Tebubio ref. 282T37442). Aspergillin PZ is a fungal metabolite originally isolated from A. awamori. It induces morphological deformation of P. oryzae conidia when used at a concentration of 89 nM. Aspergillin PZ is active against S. epidermidis (MIC = 20 μM) but not S. aureus, E. coli, or B. cereus (MICs = >20 μM). It is cytotoxic to HL-60 promyelocytic leukemia cells (IC50 = 56.61 μM) but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells (IC50s = >80 μM).

Aspochalasin D (Legacy Tebubio ref. 282T37443). Aspochalasin D, a co-metabolite originally isolated from A. microcysticus along with aspochalasins A, B, and C, has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml. Aspochalasin D is more cytotoxic via apoptosis to Ba/F3-V12 cells in an IL-3-free medium [IC50 = 0.49 μg/ml] than in an IL-3-containing medium [IC50 = 1.9 μg/ml].

Aranorosin (Legacy Tebubio ref. 282T37444). Aranorosin is a fungal metabolite originally isolated from P. roseus. It has antimicrobial activity against B. subtilis, A. niger, and C. albicans when used at a concentration of 1 mg/ml. Aranorosin also reduces viability in apoptosis-resistant HeLa/Bcl-2 cells.

Etanercept (Legacy Tebubio ref. 282T37445). Etanercept is a fusion protein consisting of the soluble portion of the p75-tumor necrosis factor receptor (TNFR) and the Fc fragment of human IgG1 and is commonly used to treat patients with rheumatoid arthritis.[1]

GGTI-2154 (Legacy Tebubio ref. 282T37446). GGTI-2154 is a potent, selective geranylgeranyltransferase I (GGTase I) inhibitor, boasting an IC50 of 21 nM and demonstrating over 200-fold selectivity against FTase (IC50=5600 nM). Its efficacy and specificity make it a valuable tool for cancer research[1][2].

UZH1 (Legacy Tebubio ref. 282T37447). UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor with an IC50 of 280 nM, while UZH1b (IC50=28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes, has antitumor activity, and serves as a chemical probe for studying METTL3[1].