A selective cell-permeable inhibitor of non-muscle myosin II ATPases, inhibiting Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC₅₀ = 0.5-5.0 μM), while poorly inhibiting smooth muscle myosin (IC₅₀ = 80 μM).

A cell-permeable, cGMP analog that activates cGMP-dependent protein kinase.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

A potent activator of KCNQ1 (Kv7.1) channels (EC₅₀ = 260 nM); EC₅₀ > 30 µM for KCNQ2, KCNQ4, and hERG; potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments IKs current in cultured…

CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1…

A photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration; also inhibits autophagosome formation by directly targeting and modifying p62, a scaffold and adaptor protein that binds both…

A selective inhibitor of JAK1 (IC₅₀ = 629 nM) that displays 30-fold selectivity for JAK1- over JAK2-dependent signaling in human whole blood; blocks IL-6/STAT1 and IL-2/STAT5 signaling in cell models and whole blood assays.

A cell-permeable inhibitor of JMJD2E (KDM4DL; IC₅₀ = 920 nM); reduces the expression of immediate early genes of HSV (IC₅₀ = ~10 µM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice.

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.

A cell-penetrating peptide inhibitor of calpain (IC₅₀ = 5 nM) which completely abolishes calpain activity in platelets; also a potent inhibitor of cathepsin K (IC₅₀ = 0.11 nM).

A naturally occuring terpenoid that potently inhibits MAGL (IC₅₀ = 93 nM); at 1 µM, significantly inhibits endogenous MAGL in isolated rat neurons.

A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

A Ca2+-selective ionophore for biological membranes that can be used in microelectrodes for the determination of resting Ca2+-activities and of slowly changing Ca2+ levels.

DPI is an irreversible inhibitor of iNOS and eNOS with IC₅₀ values of 50 nM and 0.3 µM, respectively. This inhibition is potent, irreversible, and time and temperature dependent. NADPH, NADP+, and 2'5'-ADP block the inhibitory action of DPI. Similarly, FAD or FMN protect…

A protopanaxadiol that has diverse in vitro and in vivo effects, including cardioprotective, neuroprotective, and anti-inflammatory actions.

An ER agonist that binds to ERα and ERβ with Ki values of 27.4 and 15.4 nM, respectively; demonstrates higher ER agonist activity at ERα compared to ERβ (EC50 = 66 and 330 nM, respectively).

A quinazolinone derivative that selectively inhibits dynamin GTPase activity in yeast and mammalian cells (IC₅₀ = 1-10 μM); prevents apoptosis by inhibiting mitochondrial outer membrane permeabilization.

A potent inhibitor of iNOS (IC₅₀ = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC₅₀ = 350 μM).

A biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.

A potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of PRC2; blocks trimethylation of the PRC2 target H3K27 (IC₅₀ = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.

A naturally-occurring sterol and biosynthetic precursor of several animal, fungal, and protozoan steroids, including cholesterol and ergosterol.

Reacts with thiols resulting in an increase in fluorescence intensity of up to 120-fold; the response is selective for thiols, occurs in aqueous media, and results in a fluorophore with emission at 623 nm; cell-permeable.

An antagonist of lipid A activation of TLR4 (IC₅₀ =1.68 μM), in a cell-based assay; significantly improves survival of mice given intraperitoneal LPS.

A small molecule inhibitor of KCNJ1 (IC₅₀ = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 µM; has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 µM.

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

A competitive inhibitor of nucleotide binding by Ras-related GTPases; binds Rab7 (Ki = 13 nM), preventing BODIPY-linked GTP and GDP binding with EC₅₀ values of 11.2 and 21 nM, respectively.

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC₅₀s = 15-17 nM) that spares the wild-type form of the receptor (IC₅₀ = 480 nM). AZ 5104 displays a similar overall…

A cyclic polypeptide-containing anticancer antibiotic that binds to DNA and blocks transcription by interfering with RNA synthesis; ~10 nM promotes cell death in a variety of tumors.

A hepatic metabolite of zearalenone that is a less potent agonist of estrogen receptors than the parent compound.

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5