An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

A third generation inhibitor of p38 MAP kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively); inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.

An irreversible, mechanism-based inhibitor of LSD1 (IC₅₀ = 16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC₅₀s <5 nM).

A thiol-reactive probe that can be used to label proteins at cysteine residues.

An analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively); significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2.

A verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.

An inhibitor of ferroptosis induced in MEFs by Gpx4 deletion (IC₅₀ = 22 nM) or by the ferroptosis inducers BSO, erastin, and RSL3; does not interfere with apoptosis, necroptosis, or necrosis; effectively suppresses ferroptosis in vivo when administered intraperitoneally.

A form of polymyxin B which terminates with 6-methyloctanamide; comparable to other B polymyxins in its ability to kill P. aeruginosa, A. baumannii, and K. pneumoniae isolates.

An inhibitor NF-κB activation in vitro and in vivo (IC₅₀ = 5 µM).

A second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

A natural anthocyanidin.

11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 µg/kg.

A naturally-occurring but uncommon form of sphingosine, accounting for approximately 13% of the sphingosine in human skin; can be phosphorylated by sphingosine kinases to produce C-17 sphingosine-1-phosphate.

A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

An inhibitor of STAT3 transcription factor activation, dimerization, and gene transcription; suppresses IL-6-induced phosphorylation of STAT3 in T cells (IC₅₀ = 38 μM) and is protective against angiotensin II-induced vascular dysfunction.

A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

An inhibitor of the yeast PITP Sec14, blocking both Sec14-mediated transfer of [3H]-PtdIns in vitro and growth (IC₅₀s = 0.21 and 2.87 µM, respectively).

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

A synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC₅₀ = 6 nM) and in vivo.

A divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.

Epoxyeicosatrienoic acid (EpETrE; EET) metabolites of arachidonic acid such as 11(12)-EET and 14(15)-EET have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EETs to the corresponding dihydroxy…

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 40 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; promotes stem cell differentiation.

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.

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

CAS Number: 745046-84-8 Synonyms: Ivachtin Molecular Formula: C₂₀H₂₁N₃O₇S

The main saponin constituent of C. asiatica that has been shown to improve wound healing including increasing collagen synthesis and elevating antioxidant levels in various normal and diabetic wound models.

The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by synthesis of diffusible acylhomoserine lactone (AHL) molecules. C6-HSL is a small diffusible signaling molecule involved in quorum sensing, controlling gene…

A potent inhibitor of PI3K isoforms α, δ, and γ (IC₅₀s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo.

Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1)…