A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

A water soluble and metabolically stable curaxin that activates p53 with an EC₅₀ value of 0.37 µM and inhibits NF-κB with an EC₅₀ of 0.47 µM; has broad anticancer activity in mice when administered orally.

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

A potential metabolite of bimatoprost when administered to animals; potential minor impurity in commercial preparations of bimatoprost.

A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM); bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model; decreases hepatic necrosis and apoptosis after orthotopic liver transplantation in rats.

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC₅₀ = 460 nM).

A specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

A protopanaxatriol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-diabetic actions; protects against DNA damage and apoptosis induced by ultraviolet light.

11β-PGE1 is an epimerized form of PGE1 at the C-11 position. 11β-PGE1 is a less potent isomer of PGE1. It is 13% and 3.6% as potent as PGE1 in contracting the rat uterus and guinea pig ileum, respectively.

An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). Boswellic acids are specific, non-redox inhibitors of leukotriene synthesis via 5-lipoxygenase that demonstrate anti-inflammatory…

A cell-permeable derivative of 2-HG.

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

C-6 ceramide is a cell-permeable analog of naturally occurring ceramides. With a longer carbon chain than C-2 ceramide, it is somewhat more hydrophobic, and may more closely mimic the effects of natural ceramides. C-6 ceramide mediates many diverse biological activities including apoptosis,…

A natural anthocyanidin.

Produced from Ins(1,2,3,5,6)P5 via a minor enzymatic phytate degradation pathway by K. terrigena; moderately effective in opening calcium channels relative to Ins(1,4,5)P3.

A dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC₅₀s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively); improves glucose homeostasis in diet-induced insulin resistant mice.

Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C₁₈H₂₁N₃OS

A metabolite of thyroid hormone.

Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…

A cell permeable sulfonamide-based hydroxamic acid that binds to the active site of MMP-3 (Ki = 23 nM) and prevents its activity; inhibits mouse macrophage metalloelastase MME/MMP-12 (IC₅₀ = 13 nM).

An enantiomer of atorvastatin that has little or no inhibitory activity against HMG-CoA reductase.

An inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.

An inactive metabolite of artemisinin.

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

TTP 22 is a thienopyrimidine compound that inhibits casein kinase 2 (CK2) with an IC₅₀ value of 100 nM (Ki = 40 nM). It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.

A pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base, which is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal negative control molecule.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…