Biologically Active Small Molecules, Chemicals, 25 mg
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VX-702
Cayman ChemicalA 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.
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GSK-LSD1 (hydrochloride)
Cayman ChemicalAn irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s <5 nM).
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Liproxstatin-1
Cayman ChemicalAn 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.
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D-erythro-Sphingosine C-17
Cayman ChemicalA 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.
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S3I-201
Cayman ChemicalAn 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.
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BYL719
Cayman ChemicalA 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.
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SMI-481
Cayman ChemicalAn 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).
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Tadalafil
Cayman ChemicalA 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.
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HE-3235
Cayman ChemicalA 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.
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A-23187
Cayman ChemicalA 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.
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CUDA
Cayman ChemicalEpoxyeicosatrienoic 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…
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IWP-3
Cayman ChemicalAn 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.
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N-hexanoyl-L-Homoserine lactone
Cayman ChemicalThe 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…
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Arachidonoyl-1-thio-Glycerol
Cayman ChemicalA thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.
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FSLLRY-amide
Cayman ChemicalA peptide antagonist of PAR2 which blocks activation by trypsin (IC50 = ~50 μM) but not by the synthetic agonist SLIGRL-NH2; does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein; used to study PAR2 action in cells and in animals.
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Afuresertib (hydrochloride)
Cayman ChemicalA selective, orally bioavailable inhibitor of Akt1, 2, and 3 (Kis = 0.08, 2, and 2.6 nM, respectively); inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies.
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CAY10571
Cayman ChemicalAn analog of SB203580, the highly specific pyridinylimidazole inhibitor of p38 MAPK; inhibits IL-1 production in the human monocytic cell line THP (IC50 = 0.20 µM) and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity (IC50 = 0.03 µM).
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CAY10508
Cayman ChemicalA potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.
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1-Palmitoyl Lysophosphatidic Acid
Cayman ChemicalAn LPA analog containing palmitic acid at the sn-1 position.
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CYM 5442
Cayman ChemicalA selective SIP1 agonist (EC50 = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC50 = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.
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Alfuzosin (hydrochloride)
Cayman ChemicalA post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia; displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B,…
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ABT-263
Cayman ChemicalA potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, like Bim, leading to apoptosis; induces apoptosis in cancer cell lines expressing mutants of β-catenin 1.
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Estradiol 17-(ß-D-Glucuronide) (sodium salt)
Cayman ChemicalAn estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.
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Darapladib
Cayman ChemicalA reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM) that produces sustained inhibition of plasma Lp-PLA2 activity in humans.
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PD 153035 (hydrochloride)
Cayman ChemicalA highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC50 = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.
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GSK2578215A
Cayman ChemicalGSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…
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DC4 Crosslinker
Cayman ChemicalA MS-cleavable crosslinking reagent (18Å in length) that contains two intrinsic positive charges, which allow cross-linked peptides to fragment into their component peptides by collision-induced dissociation or in-source decay.
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(-)-Blebbistatin
Cayman ChemicalA 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).
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Nevirapine
Cayman ChemicalA 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).
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Nobiletin
Cayman ChemicalA 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).
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ML-277
Cayman ChemicalA 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…