Bioactive Small Molecules
Cayman Chemical ANTIBODY ABT-639 1mg
A T-type calcium channel blocker; inhibits inactivated-state Cav3.2 channels (IC50 = 2.3 μM) and inactivated-state Cav3.1 and Cav3.3 channels by 50 and 39%, respectively, at 10 μM; selectively inhibits inactivated-state T-type calcium currents over resting-state currents in rat DRG neurons (IC50s = 7.6 and >30 μM, respectively); reverses the hind limb grip force deficit in a rat model of MIA-induced osteoarthritic pain (ED50 = 2 mg/kg); dose-dependently increases the paw withdrawal threshold in rat SNL and CCI models of neuropathic pain; attenuates cold allodynia in the CCI rat model at ≥3 mg/kg
Medchemexpress LLC Taspoglutide | 275371-94-3 | 98.4% | 3339.71 | 1 MG
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist. It was developed for the treatment of type 2 diabetes and has an EC50 value of 0.06 nM. It activates the GLP-1 receptor with comparable affinity and potency to the natural ligand for the hGLP-1 receptor. Taspoglutide enhances glucose-induced insulin secretion and lowers blood glucose in models of type 2 diabetes.
- Activates GLP-1 receptor
- Enhances glucose-induced insulin secretion
- Lowers blood glucose
- Suitable for type 2 diabetes research
Medchemexpress LLC GRGDSP TFA | 98.0% | 701.61 | 10 MG
GRGDSP TFA is an integrin inhibitor. This synthetic linear RGD peptide is used as a soluble integrin-blocking agent in research.
- Inhibits the adherence of tumor cells to endothelial cells of blood vessels.
- Limits tumor metastasis.
- Utilized with other RGD peptides in integrin research.
- Modifies cardiovascular implant surfaces to promote endothelialization.
Cayman Chemical ChLRmethIazolehydrochLRId 5mg
A potentiator of GABAA receptors; potentiates GABA-induced currents in L-M(TK-) cells expressing α1β1γ2 or α1β2γ2 subunit-containing GABAA receptors (EC50s = 0.8 and 3.4 µM, respectively); protects against MES-induced seizures in mice (ED50 = 130.8 mg/kg); reduces infarct volume in a permanent rat model of MCAO-induced focal ischemia
Cayman Chemical QuercetIn-7-OD-Glucopyrno 5mg
A flavonoid; has antioxidant activity in a ORAC assay and decreases tert-butyl hydroperoxide-induced ROS in L-929 cells at 0.25 and 1 UG/ml; reduces protein levels of iNOS and COX-2 in LPS-stimulated RAW 264.7 cells at 15 and 30 UG/ml; decreases angiogenesis in isolated rat aortic rings and proliferation of HUVECs but has no effect on tube formation or chemotaxis of HUVECs at 100 µM
Medchemexpress LLC Purmorphamine | 483367-10-8 | C31H32N6O2 | 100 MG
Purmorphamine is a potent smoothened/Smo receptor agonist with an EC50 of 1 μM and an IC50 of 1.5 μM for Smoothened. It is intended for research use only and not for human or animal therapeutic use. This compound promotes osteoblast differentiation and up-regulates key markers of the osteoblast phenotype, demonstrating its utility in studying bone development and related cellular processes.
- Acts as a smoothened/Smo receptor agonist
- Induces osteoblast differentiation
- Up-regulates alkaline phosphatase activity and RUNX-2 expression
- Up-regulates osteocalcin at specific doses
- Induces STAT3 phosphorylation
- Promotes bone-like nodule formation in human bone marrow mesenchymal cells
- Significantly decreases cell numbers in combination with sirolimus
Cayman Chemical ANTIBODY DAR-4M 1mg
A fluorescent probe for the detection of NO; fluorescence intensity of DAR-4M increases with increasing NO concentration, however, the fluorescent yield can be increased further in the presence of both NO and other RNS, but not in the presence of non-NO RNS alone; upon oxidation, it is converted to DAR-4M T, which displays abs/em = 554/572 nm, respectively
Medchemexpress LLC GNE-272 | 1936428-93-1 | MFCD30738051 | 99.6% | 424.47 g·mol⁻¹ | C22H25FN6O2 | 100 MG
GNE-272 is a potent, selective small-molecule probe that targets the bromodomains of CBP and EP300. It exhibits low-nanomolar biochemical potency and shows cellular activity including inhibition of MYC expression, making it suitable for in vitro and in vivo probe studies when handled as a research-grade compound.
- Potent CBP/EP300 bromodomain inhibition (CBP IC50 0.02 μM, EP300 IC50 0.03 μM).
- Lower affinity for BRD4 (IC50 13 μM).
- Demonstrated cellular activity (MV4-11 MYC inhibition EC50 1.9 μM).
- High reported purity (99.6%).
- Supplied as powder and as DMSO solution for ready reconstitution.
- Storage stability data provided for powder and solvent forms.
Cayman Chemical ANTIBODY HT-2157 5mg
A GAL3 receptor antagonist (Ki = 17 nM); selective for GAL3 over GAL1 and GAL2 (Kis = >10 µM for both); induces apoptosis in various cell types, including HL-60 leukemia and BV-2 murine microglial cells, as well as isolated human PBMCs at 10 µM; decreases operant alcohol, sucrose, and saccharin self-administration in rats at 30 mg/kg; increases drinking in the Vogel punished drinking task and reduces immobility time in the forced swim test in rats, indicating anxiolytic- and antidepressant-like activities, respectively, at 3 and 10 mg/kg
Medchemexpress LLC Decapeptide-12 | 137665-91-9 | 99.9% | 1395.52 | 10 MG
Decapeptide-12 is a small oligopeptide and a tyrosinase inhibitor that interacts with the C-terminal residue of tyrosinase (Kd: 61.1 μM). It is a competitive inhibitor of mushroom tyrosinase (IC50: 40 μM) and also increases the transcription of SIRT. It reduces melanin content in melanocytes and is used for research in melanogenesis, senescence, and inflammation.
- Tyrosinase inhibitor
- Reduces melanin content in melanocytes
- Increases transcription of SIRT
- Used for research of melanogenesis, senescence, and inflammation
- Soluble in H2O (≥ 100 mg/mL or 71.66 mM)
Cayman Chemical ApIgenIn 7-glucosIde 5mg
A flavonoid with anti-inflammatory and anxiolytic activities; inhibits LPS-induced nitric oxide production in RAW 264.7 cells from 0.16-10 μM; reduces pulmonary edema and lung inflammation in a mouse model of LPS-induced acute lung injury at 10 mg/kg; increases the number of entries and the time spent in the open arms of the elevated plus maze in rats
Medchemexpress LLC Dynorphin A (1-10) (TFA) | 98.6% | 1348.48 | 10 MG
Dynorphin A (1-10) (TFA) is an endogenous opioid neuropeptide that binds to extracellular loop 2 of the κ-opioid receptor. It also blocks NMDA-activated current with an IC50 of 42.0 μM. Studies show that Dynorphin A (1-10) (TFA) blocks NMDA-activated currents in a voltage-independent manner.
- Endogenous opioid neuropeptide
- Binds to extracellular loop 2 of the κ-opioid receptor
- Blocks NMDA-activated current
- IC50 of 42.0 μM for NMDA receptor blockade
- Voltage-independent action on NMDA receptors