Bioactive Small Molecules
Cayman Chemical LY379268, Purity: ≥99%, CAS: 191471-52-0, 1 mg
A group II mGluR inhibitor (EC50s = 2.69 and 4.48 nM, respectively for mGluR2 and mGluR3); over 80-fold selectivity over group I and III mGluRs; no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM; raises extracellular dopamine level in the prefrontal cortex to 168% basal level in treated rats (3 mg/kg)
Medchemexpress LLC Umifoxolaner | 2021230-37-3 | 99.97% | 643.86 | 1 MG
Umifoxolaner (ML-878) is a γ-aminobutyric acid (GABA) regulated chloride channels antagonist. It functions as an anti-parasitic agent.
- Functions as a GABA regulated chloride channels antagonist
- Acts as an anti-parasitic agent
AdipoGen Remdesivir (100 mg)
Chemical. CAS: 1809249-37-3. Formula: C27H35N6O8P. MW: 602.6. Remdesivir is a adenosine triphosphate analog with broad-spectrum antiviral activity. It is a prodrug that metabolizes into its active form GS-441524. GS-441524 is an adenosine nucleotide analog in viral RNA production. It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase and evades proofreading by viral exoribonuclease (ExoN), causing a decrease in viral RNA production (RNA synthesis arrest), either by terminating RNA chains or causing mutations. It inhibits MERS-CoV or SARS-CoV-infected HAE cultures (EC50=74nM and 69nM) and murine hepatitis virus (MHV) (EC50=30nM). Remdesivir is effective in the control of 2019-nCoV (COVID-19) infection in vitro. It now also has been studied as potential treatment of SARS-CoV-2 infections.
Cayman Chemical BPH-1358, Purity: ≥95%, CAS: 5352-53-4, 25 mg
An inhibitor of UPPS (IC50 = 0.11 µM for the E. coli and S. aureus enzymes) and FPPS (IC50 = 1.8 µM for the human enzyme); active against E. coli and S. aureus (EC50s = 0.3 and 0.29 nM, respectively); increases survival in a mouse model of S. aureus infection at 10 mg/kg
Medchemexpress LLC Gap 27 | 198284-64-9 | 99.9% | 1304.53 | 5 MG
Gap 27 is a synthetic connexin43 mimetic peptide and a gap junction inhibitor. It has conserved sequence homology to a portion of the second extracellular loop leading into the fourth transmembrane connexin segment.
- Significantly reduces the number and activity of TRAP-positive mononuclear and multinucleated rat osteoclasts cultured on bovine bone slices
- Diminishes the resorbed area
- Inhibits acetylcholine-induced, endothelium-dependent hyperpolarizations in the guinea-pig isolated internal carotid artery
- Inhibits relaxation in the thoracic aorta and superior mesenteric artery
- Attenuates the endothelium-dependent component of ATP-induced relaxation in the thoracic aorta
Cayman Chemical CS 2100, Purity: ≥98%, CAS: 913827-99-3, 50 mg
An S1P1 agonist; selectively induces GTPγS binding in CHO-K1 cells expressing human or rat S1P1 (EC50s = 4 and 1.5 nM, respectively) over those expressing human or rat S1P3 (EC50s = >20 and 7.4 µM, respectively); transiently reduces blood lymphocyte levels in rats with the levels returning to baseline within 24-48 hours at 0.1 and 1 mg/kg; reduces hind paw volume in a rat model of adjuvant-induced arthritis (ID50 = 0.44 mg/kg); decreases severity in a mouse model of EAE at 0.3 and 1 mg/kg
Cayman Chemical MLN120B, Purity: ≥98%, CAS: 783348-36-7, 25 mg
An IKKβ inhibitor (IC50 = 45 nM); selective for IKKβ over a panel of 30 tyrosine and serine/threonine kinases (IC50s = >50 µM for all); inhibits TPA-induced NF-κB activation (IC50 = 2.8 µM in a reporter assay); inhibits proliferation in a panel of six multiple myeloma cancer cell lines; reduces serum levels of soluble human IL-6 receptor in a SCID-hu mouse model of bone marrow-engrafted INA-6 multiple myeloma at 50 mg/kg; reduces paw swelling, as well as cartilage destruction and bone erosion in the inflamed joints, in a rat model of CFA-induced rheumatoid arthritis (MED = 12 mg/kg)
![Medchemexpress LLC N-[2-[N'-pentyl-(6,6-dimethyl-2,4-heptadiynyl)amino]ethyl]- (2-methyl-1-naphthylthio)acetamide | 138046-43-2 | 100.0% | 452.63 g·mol⁻¹ | C31H36N2O | 50 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000239848.png-250.jpg)
Medchemexpress LLC N-[2-[N'-pentyl-(6,6-dimethyl-2,4-heptadiynyl)amino]ethyl]- (2-methyl-1-naphthylthio)acetamide | 138046-43-2 | 100.0% | 452.63 g·mol⁻¹ | C31H36N2O | 50 MG
YM-750 is a small-molecule inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with a reported IC50 of 0.18 μM. Supplied as a high-purity solid, it is used in biochemical and cell-based research to investigate cholesterol esterification and cellular lipid metabolism.
- Potent ACAT inhibitor (IC50 = 0.18 μM) for biochemical assays.
- High purity suitable for research (reported 99.95%).
- Solid powder formulation for accurate weighing and handling.
- Storage recommendations provided for long-term stability (powder: -20°C).
- Available in multiple research-scale pack sizes, including 50 mg.
- Applicable to studies of cholesterol esterification and lipid metabolism.
TARGETMOL CHEMICALS INC ADAGRASIB 25MG
Also available in 10 mg 50 mg 100 mg 500 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Adagrasib (MRTX849) is a potent selective and covalent KRASG12C inhibitor with potential antineoplastic activity. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling. purity: 99%
Cayman Chemical MC70, Purity: ≥98%, CAS: 1031367-64-2, 10 mg
A P-gp inhibitor; inhibits the efflux of [3H]vinblastine by ABCB1 in Caco-2 colon cancer cells (EC50 = 0.05 µM); inhibits the efflux of rhodamine-123 and calcein-AM by BCRP and MRP1 in MDCK cells (EC50s = 73 and 9.3 µM, respectively); enhances growth inhibition of MCF-7/ADR breast cancer cells at 2 or 20 µM when used in combination with doxorubicin in vitro, but does not alter the effectiveness of doxorubicin on growth inhibition in Caco-2 cells; increases phosphorylation of p38 and JNK in Caco-2 cells and MCF-7/ADR cells when used at a concentration of 20 µM
![AdipoGen Ixazomib citrate [MLN9708] (25 mg)](https://assets.fishersci.com/TFS-Assets/CCG/product-images/502054053.PNG-250.jpg)
AdipoGen Ixazomib citrate [MLN9708] (25 mg)
Chemical. CAS: 1239908-20-3. Formula: C20H23BCl2N2O9. MW: 517.1. Synthetic. Potent selective and reversible proteasome inhibitor (all proteolytic subunits). Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=3.4nM). Cross-reacts and inhibits the trypsin-like beta2 subunit (IC50=3.5µM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=0.03µM). Anticancer compound effective in cell-based assays, in xenografts and against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma. Prodrug that rapidly hydrolyzes to MLN2238 (AG-CR1-3670). Exhibits improved pharmacodynamics and antitumor activity compared to bortezomib in various B-cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models.
Medchemexpress LLC MK-0752 | 471905-41-6 | 99.35% | 442.90 | 100 UG
MK-0752 is a potent, orally active, and specific γ-secretase inhibitor. It demonstrates a dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 is capable of crossing the blood-brain barrier and reduces newly generated CNS Aβ in vivo. It is for research use only.
- Potent, orally active, and specific γ-secretase inhibitor.
- Dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells.
- Crosses the blood-brain barrier.
- Reduces newly generated CNS Aβ in vivo.
Cayman Chemical KW 2478, Purity: ≥98%, CAS: 819812-04-9, 10 mg
An Hsp90 inhibitor (IC50 = 3.8 nM for Hsp90α); inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin's lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively); decreases expression of IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells; reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model at 100 mg/kg
Cayman Chemical VL285, Purity: ≥98%, CAS: 1448188-57-5, 5 mg
A starting material that has been used in the synthesis of PROTACs
Medchemexpress LLC GPR84 antagonist 2 | 2244269-74-5 | 99.1% | C28H16Cl2NaO4PS2 | 10MG
GPR84 antagonist 2 is a potent, selective, and orally active antagonist of the G protein-coupled receptor GPR84, reported with an IC50 of 8.95 nM. The compound has demonstrated activity in calcium mobilization assays and can inhibit chemotaxis of neutrophils and macrophages, supporting its use in research on inflammatory pathways such as ulcerative colitis.
- Potent and selective GPR84 antagonism (IC50 = 8.95 nM).
- Demonstrated activity in calcium mobilization assays.
- Inhibits chemotaxis of neutrophils and macrophages upon receptor activation.
- Suitable for in vitro and in vivo research into inflammatory pathways.
- Available as solid and DMSO solution formats for experimental flexibility.