Bioactive Small Molecules
Cayman Chemical ANTIBODY CAY10753 5mg
A TNKS2 inhibitor (IC50 = 0.3 nM); selective for TNKS2 over TNKS1 (IC50 = 6.1 nM), as well as PARP1 and PARP2 (IC50s = 89.6 and 37.8 nM, respectively); inhibits proliferation of DLD-1 cells at 1 µM
Medchemexpress LLC GNE-781 | 1936422-33-1 | 98.5% | 525.59 | 10 MG
GNE-781 is an orally active, highly potent, and selective CBP inhibitor with an IC50 of 0.94 nM in a TR-FRET assay. It also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. It has demonstrated antitumor activity in an MOLM-16 AML xenograft model. GNE-781 is a potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) and is highly selective for CBP/P300.
- Orally active
- Highly potent and selective CBP inhibitor
- Inhibits BRET and BRD4(1)
- Displays antitumor activity in an MOLM-16 AML xenograft model
- Reduces FOXP3 (forkhead box P3) transcript levels
- Exquisitely selective for CBP/P300
- Decreases Foxp3 transcript levels in a dose-dependent manner in vivo
- Suppresses MYC in vivo
Cayman Chemical Apararenone 5mg
A non-steroidal mineralocorticoid receptor antagonist (Ki = 0.104 µM for the human receptor); selective for mineralocorticoid receptors over ERα and ERβ and glucocorticoid, progesterone, and androgen receptors (IC50s = >100 µM for all); increases the urinary ratio of sodium to potassium in adrenalectomized rats; inhibits aldosterone- and nephrectomy-induced increases in systolic blood pressure and urinary albumin levels, as well as myocardial necrosis and fibrosis, cardiac arterial degeneration, and renal tubule damage, in a rat model of renal hypertension at 3 or 10 mg/kg per day
Medchemexpress LLC PD 128907 hydrochloride | 112960-16-4 | MFCD00210210 | 99.5% | 285.77 | C14H20ClNO3 | 10 MG
PD 128907 hydrochloride is the hydrochloride salt of a potent and selective dopamine D3 receptor agonist intended for in vitro pharmacology and receptor-binding research. The material is supplied with a high stated purity and defined chemical characterization suitable for laboratory assays.
- Selective dopamine D3 receptor agonist with reported EC50 of 0.64 nM.
- High purity (99.51%).
- Molecular weight 285.77 and molecular formula C14H20ClNO3.
- Suitable for in vitro receptor binding and functional assays.
- Available in multiple small-scale milligram pack sizes for laboratory use.
Cayman Chemical ANTIBODY GSK2983559 10mg
A RIPK2 inhibitor; inhibits RIPK2 by 65% in a kinase assay at 10 µM; inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60-89% in a panel of 344 kinases at 10 µM; reduces colonic damage in a mouse model of TNBS-induced colitis at 7.5 and 145 mg/kg twice per day; a prodrug
Medchemexpress LLC 1,2-diheptanoyl-sn-glycero-3-phosphocholine | 39036-04-9 | 99.5% | 50 MG
1,2-diheptanoyl-sn-glycero-3-phosphocholine is a synthetic short-chain phosphatidylcholine used as a lipid detergent and model membrane component in biochemical and biophysical research. It has defined molecular properties and is supplied at high purity for laboratory applications.
- Short-chain phosphatidylcholine suitable for micelle formation and membrane mimetics.
- High purity for analytical and biophysical assays.
- Defined molecular weight and formula for accurate stoichiometry.
- Available in multiple small pack sizes for lab-scale experiments.
- Compatible with common organic solvents for lipid dispersion preparation.
Medchemexpress LLC C16-PAF | 74389-68-7 | 99.86% | 523.68 | 50 MG
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
- Phospholipid mediator.
- Platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR).
- Exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR.
- Potent MAPK and MEK/ERK activator.
- Induces increased vascular permeability.
- For research use only.
Medchemexpress LLC Serabelisib (MLN1117) | 1268454-23-4 | 99.4% | 50 MG
Serabelisib (MLN1117) is a selective PI3Kα (p110α) inhibitor supplied as a high-purity solid for biochemical and cell-based research applications.
- Selective PI3Kα inhibitor with reported p110α IC50 of 15 nM.
- High purity (99.4%).
- Molecular formula C19H17N5O3 and molecular weight 363.37.
- Supplied in small-scale solid quantities suitable for assay development and preclinical studies.
- Recommended storage: powder at -20 °C (long term) or 4 °C (short term); in solvent at -80 °C.
Medchemexpress LLC 3-Azetidinamine, 1-(8-bromopyrido[2,3-e]tetrazolo[1,5-a]pyrazin-4-yl)-N-methyl- | 1429375-54-1 | 99.8% | 335.16 | 25 MG
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. It does not show any noticeable binding affinity to other subtypes of histamine receptors (H1R, H2R, and H3R).
- Potent and highly selective H4 receptor antagonist
- Does not bind to H1R, H2R, and H3R
- Shows significant antipruritic and anti-inflammatory efficacy
- Available as a light yellow to yellow solid
- Provides stable storage for both powder and solution
- Soluble in various in vitro and in vivo dissolution protocols
Medchemexpress LLC Pf-06795071 | 2075629-81-9 | 99.31% | 399.34 | 25 MG
PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM. It shows excellent selectivity against FAAH. This product is suitable for various laboratory applications including neuroinflammation research.
- Potent and selective covalent MAGL inhibitor
- IC50 of 3 nM against MAGL
- Excellent selectivity against FAAH
- White to off-white solid appearance
Medchemexpress LLC HDAC8-IN-1 | 1417997-93-3 | 99.8% | 345.39 | 25 MG
HDAC8-IN-1 is a highly selective inhibitor of Histone Deacetylase 8 (HDAC8) with an IC50 of 27.2 nM. It demonstrates antiproliferative effects in human lung cancer cell lines such as A549, H1299, and CL1-5, and exhibits cytotoxicity against human lung CL1-5 cells without significant cytotoxicity towards normal IMR-90 cells. This compound has also been observed to slightly reverse IL-4-induced Foxp3 repression, acting similarly to a class I HDAC inhibitor.
- Potent inhibitor with an IC50 of 27.2 nM.
- Shows antiproliferative effects in various human lung cancer cell lines.
- Exhibits selective cytotoxicity against human lung CL1-5 cells, with minimal impact on normal IMR-90 cells.
- Can slightly reverse IL-4-induced Foxp3 repression and promote regulatory T cell differentiation.
Medchemexpress LLC Nisoxetine (hydrochloride) | 57754-86-6 | 99.92% | 10 MM * 1 ML
Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET) with a Kd of 0.76 nM. It is an antidepressant and local anesthetic that can block voltage-gated sodium channels.
- Potent and selective inhibitor of noradrenaline transporter (NET)
- Kd of 0.76 nM (NET)
- Antidepressant
- Local anesthetic
- Blocks voltage-gated sodium channels
Medchemexpress LLC Tizaterkib | 2097416-76-5 | MFCD31631580 | 99.1% | 494.50 | 25 MG
Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor, with an IC50 of 0.6 nM. It is intended for research use only and not for patients.
- Potent and selective ERK2 inhibitor
- Inhibits the growth of cancer cell lines with KRAS mutations as monotherapy
- Enhances effect synergistically when combined with Selumetinib
- Reduces tumor growth in A549 xenograft models in combination with MEK inhibitor Selumetinib