Biologically Active Small Molecules, 100 mg, Chemicals
-
Rosiglitazone
Cayman ChemicalA potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.
-
DPPH
Cayman ChemicalA cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.
-
Necrostatin-1
Cayman ChemicalAn inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells with an EC50 value of 490 nM.
-
Lenalidomide
Cayman ChemicalAn analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.
-
Suramin (sodium salt)
Cayman ChemicalA polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of…
-
Monobromobimane
Cayman ChemicalA thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.
-
PIT-1
Cayman ChemicalA selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding (IC50 = 31 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).
-
Imatinib (mesylate)
Cayman ChemicalA first generation tyrosine kinase inhibitor that is used in the treatment of CML, GIST, and other cancers; selectively targets certain tyrosine kinases, including c-ABL, PDGFR, KIT, and the oncoprotein BCR-ABL.
-
Levosimendan
Cayman ChemicalA calcium sensitizer that causes increased cardiac contractility by binding troponin C (EC50 = 9 nM), promotes vasodilation by activating ATP-sensitive potassium channels on vascular smooth muscle cells (EC50 = 0.28 µM), and performs a cardioprotective function by…
-
FeTMPyP
Cayman ChemicalFeTMPyP is a synthetic porphyrin complexed with iron, which acts as a peroxynitrite decomposition catalyst. The rate constant for decomposition of peroxynitrite by FeTMPyP is 2.2 x 106 M−1s−1 with a turnover number of 360 ± 170 s−1. The predominant product (>90%) of this…
-
Danazol
Cayman ChemicalA derivative of testosterone and ethisterone that binds androgen receptors and sex hormone-binding globulin causing a 3-fold increase in free testosterone; possesses weak androgenic effects and inhibits the production of gonadotropins.
-
a-D-Galactose-1-phosphate (potassium salt)
Cayman ChemicalAn intermediate in the interconversion of glucose and galactose.
-
DPTA NONOate
Cayman ChemicalA NO donor with a half-life of three hours at 37°C, pH 7.4; liberates two moles of NO per mole of parent compound.
-
Nitrendipine
Cayman ChemicalA dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A1, A2A, and A3 receptors with Ki values of 8.96, 23.0, and 8.3 µM, respectively.
-
Paclitaxel
Cayman ChemicalA potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…
-
2,7-Dichlorodihydrofluorescein diacetate
Cayman ChemicalA fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.
-
Tianeptine (sodium salt)
Cayman ChemicalAn atypical antidepressant with diverse actions, most notably on the glutamatergic system; attenuates glutamate release and modulates the function of AMPAR; acts as an agonist of the µ-opioid receptor (EC50s = 194 and 641 nM for human and mouse receptors, respectively).
-
(R,S)-Anatabine
Cayman ChemicalA minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.
-
Montelukast (sodium salt)
Cayman ChemicalThe CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…
-
Celecoxib
Cayman ChemicalAn anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.
-
Temozolomide
Cayman ChemicalAn imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.
-
Biotin-NHS
Cayman ChemicalA compound used to attach biotin to primary amines, such as lysines on the surface of proteins, under alkaline conditions (pH~8-9).
-
Evernic Acid
Cayman ChemicalA secondary metabolite produced by some species of lichen that binds FAS-II enzymes to produce antibacterial and antiplasmodial effects; inhibits PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei…
-
Ethyl Tricosanoate
Cayman ChemicalA long chain saturated fatty acid ethyl ester found in small quantities in liverwort, C. concium.
-
Pimonidazole
Cayman ChemicalA small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.
-
5-Azacytidine
Cayman ChemicalAn inhibitor of DNA methyltransferases that reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC50s = 2.4 and 2.6 μM for in vitro anti-myeloma activity) and cancer (IC50s ~ 0.4 μM for inhibiting proliferation of various cancer cell lines).
-
Fluphenazine-N-2-chloroethane (hydrochloride)
Cayman ChemicalA derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses…
-
Ganciclovir
Cayman ChemicalA synthetic analog of 2'-deoxy-guanosine which is used to treat or prevent cytomegalovirus (CMV) infections; inhibits the replication of human CMV with an IC50 value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.
-
Vandetanib
Cayman ChemicalA broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including VEGFR and EGFR, with IC50 values in the nanomolar range; also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.
-
DL-threo-PDMP (hydrochloride)
Cayman ChemicalA PDMP mixture containing D-threo (1R,2R) and L-threo (1S,2S) PDMP; reduces the synthesis of glucosylceramide increases cellular ceramide, and induces cell cycle arrest.
-
Pirfenidone
Cayman ChemicalAn orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.
-
Olaparib
Cayman ChemicalA potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM); can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.