Bioactive Small Molecules
Cayman Chemical BI-3802, Purity: ≥95%, CAS: 2166387-65-9, 1 mg
A Bcl-6 degrader (DC50 = 20 nM in SU-DHL-4 cells); binds to Bcl-6 in a cell-free assay and inhibits the interaction of Bcl-6 with NCOR1 in a reporter assay (IC50s = ≤3 and 43 nM, respectively); induces polymerization and SIAH1-dependent ubiquitination of Bcl-6 in cell-free assays; enhances imatinib-induced decreases in tumor volume and weight in a GIST-T1 gastrointestinal stromal tumor mouse xenograft model
Medchemexpress LLC Leptospermone 5mg | 567-75-9 | 266.33 g/mol | C15H22O4 | 5 MG
Leptospermone is a natural phytochemical and a competitive, reversible inhibitor of p-hydroxyphenylpyruvate dioxygenase (HPPD). It is used as a research reagent for HPPD inhibition studies and for investigating herbicidal bleaching activity.
- High purity (98.46%).
- Molecular weight 266.33 g/mol.
- Chemical formula C15H22O4.
- Reported IC50 for HPPD inhibition: 12.1 μM.
- Sold in small research pack sizes suitable for laboratory assays (5 mg, 10 mg, 25 mg, 50 mg).
Cayman Chemical ABX-1431, Purity: ≥98%, CAS: 1446817-84-0, 10 mg
An inhibitor of MAGL (IC50s = 14 and 27 nM for human and rat enzyme, respectively); selective for MAGL over ABHD6 and PLA2G7 (IC50s = 2.7 and >10 μM, respectively), as well as a panel of 33 serine hydrolases and a panel of 95 enzymes, receptors, transporters, and ion channels at 10 μM; selective for MAGL over CYP1A2, CYP2C9, CYP2C19, and CYP3A4/5 (IC50s = >50 μM); inhibits MAGL activity in mouse and rat brain ex vivo (ED50s = 1.4 and 0.5 mg/kg, respectively); decreases brain levels of 2-AG in mice and rats; reduces formalin-induced paw-licking time in rats
Medchemexpress LLC GSK4112 | 1216744-19-2 | 99.9% | C18H21ClN2O4S | 1 ML
GSK4112 is a Rev-erbα agonist, with an EC50 of 0.4 μM, used as a chemical tool to study Rev-erbα's role in transcriptional repression, circadian biology, and metabolic pathways. It represses bmal1 and gluconeogenesis-related gene expression in vitro, recruits HDAC3, and modulates hepatic gene expression. In vivo, it mitigates Fas-induced acute hepatic damage.
- Rev-erbα agonist (EC50 0.4 μM)
- Chemical tool for studying transcriptional repression, circadian biology, and metabolic pathways
- Represses bmal1 and gluconeogenesis-related gene expression
- Recruits HDAC3 and modulates hepatic gene expression
- Reduces glucose output in murine hepatocytes
- Mitigates Fas-induced acute hepatic damage in vivo
Cayman Chemical Droxinostat, Purity: ≥98%, CAS: 99873-43-5, 5 mg
An inhibitor of HDAC3, HDAC6, and HDAC8 (IC50s = 16.9, 2.47, and 1.46 μM, respectively); selective for HDAC3, 6, and 8 over HDAC1, 2, 7, 9, and 10 (IC50s = >20 μM); inhibits proliferation and colony formation of SMMC-7721 and HepG2 hepatocellular carcinoma cell lines via activation of mitochondrial apoptosis and reduction of c-FLIP
Cayman Chemical SPA70, Purity: ≥90%, CAS: 931314-31-7, 25 mg
A PXR antagonist (IC50 = 0.51 µM); selective for PXR over 10 additional nuclear receptors at >5 µM, as well as over a panel of 384 kinases at 10 µM; inhibits rifampicin-induced PXR activation from 0.1-10 µM; inhibits rifampicin-induced CYP3A4 activity in primary human hepatocytes; inhibits PXR agonist-induced CYP3A4-mediated metabolism of midazolam and paclitaxel in hPXR-tg mice at 200 mg/kg
Cayman Chemical MK-8745, Purity: ≥98%, CAS: 885325-71-3, 10 mg
An Aurora A kinase inhibitor (IC50 = 0.6 nM); selective for Aurora A over Aurora B kinase (IC50 = 280 nM); induces cell cycle arrest at the G2/M phase in non-Hodgkin lymphoma cells at 1 μM; induces apoptosis and polyploidy in p53-positive and -negative HCT116 colon cancer cells, respectively, at 5 μM; induces apoptosis in sarcoma, melanoma, and pancreatic cancer cell lines in a p53-dependent manner at 5 μM
Cayman Chemical Rivanicline (hydrochloride), Purity: ≥98%, 5 mg
An α4β2 subunit-containing nAChR agonist; selectively induces rubidium ion efflux in M10 cells expressing α4β2 subunit-containing nAChRs (EC50 = 0.73 µM for the chicken channels) over M10 cells expressing α3β4- or α1β1γδ subunit-containing receptors (EC50s = >1,000 nM for both for the chicken channels) and a panel of 34 receptors, ion channels, and kinases at 10 µM; induces contractions in isolated guinea pig ileum (EC30 = 15 µM); prevents scopolamine-induced memory deficits in the passive avoidance test in mice at 0.6 µmol/kg; decreases the number of errors in the radial arm maze in a rat model of ibotenic acid-induced memory impairment at 0.3, 0.6 or 1.2 µmol/kg
AdipoGen (-)-Arctiin (50 mg)
Chemical. CAS: 20362-31-6. Formula: C27H34O11. MW: 534.6. Isolated from Arctium lappa. Metabolizes into (-)-Arctigenin (AG-CN2-0530). Multifunctional natural compound with photoprotective, anti-inflammatory, antidiabetic, antiproliferative and antiviral activities. Decreasing the production of nitric oxide and pro-inflammatory cytokines, such as IL-1beta, IL-6, TNF-alpha and PGE2 through the inhibition of PI3K/AKT/NF-kappaB signaling pathway. Suppresses cyclin D1 protein expression in multiple types of human tumor cells. Inhibitor of HIV-I integrase. Inhibits adipogenesis in 3T3-L1 adipocytes through the inhibition of PPARgamma and C/EBPalpha and the activation of AMPK signaling pathways. Photoprotective agent showing UVB protection in keratinocytes, which is mediated by miRNA responses and the suppression of UVB-induced cell death. Inhibitor of STAT3 phosphorylation at tyrosine 705 residue.
Medchemexpress LLC MI-3454 | 2134169-43-8 | 98.03% | 636.73 | 100 MG
MI-3454 is an orally active, potent, and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. It inhibits proliferation, induces differentiation, and leads to leukemia regression in mouse models of MLL1-rearranged or NPM1-mutated leukemia by downregulating key genes.
- Inhibits proliferation of murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1.
- Downregulates HOXA9 and MEIS1 expression in human leukemic cell lines.
- Reduces viability of leukemic cells with MLL fusion proteins (GI50 7-27 nM).
- Blocks menin-MLL1 interaction.
- Does not potently inhibit cytochromes P450.
- Induces remission or regression of leukemia in MLL1-rearranged or NPM1-mutated mouse models.
- Exhibits favorable stability in murine and human liver microsomes.
- Shows limited ability to cross the blood-brain barrier.
Medchemexpress LLC N,O-bis(trimethylsilyl)trifluoroacetamide with trimethylchlorosilane | 25561-30-2 | MFCD00008269 | 98.0% | 257.40 g/mol | C8H18F3NOSi2 | 25G
N,O-Bis(trimethylsilyl)trifluoroacetamide with trimethylchlorosilane is a silylating reagent used to convert polar functional groups into trimethylsilyl derivatives, improving volatility and thermal stability for gas chromatography and GC-MS analysis. Supplied for research use, it is typically a colorless to light yellow liquid and is provided with documentation to support analytical workflows.
- Derivatizes hydroxyl, carboxyl, and amino functional groups.
- Improves volatility and thermal stability for GC and GC-MS analysis.
- Compatible with common chromatographic workflows and instruments.
- High purity (98.0%) for reproducible analytical results.
- Available in multiple packaging sizes to suit routine or bulk use.
- Documentation available for quality control, including SDS, COA, and NMR.
Medchemexpress LLC L-Arginine-13C hydrochloride | 94740-43-9 | 211.65 | 25 MG
L-Arginine-13C hydrochloride is the 13C-labeled form of L-Arginine hydrochloride. L-Arginine hydrochloride is a nitrogen donor for the synthesis of nitric oxide, a potent vasodilator that is often deficient during sickle cell crisis. This product is intended for research use only and is not sold to patients. Stable heavy isotopes of hydrogen, carbon, and other elements are incorporated into drug molecules primarily as tracers for quantitation during the drug development process. Deuteration, for instance, can affect the pharmacokinetic and metabolic profiles of drugs.
- Can be used as a tracer
- Functions as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS
Medchemexpress LLC Sodium 3-methyl-2-oxobutanoate-d7 | 2483831-46-3 | 145.14 | 5MG
Sodium 3-methyl-2-oxobutanoate-d7 is the deuterium-labeled form of Sodium 3-methyl-2-oxobutanoate. This compound acts as a precursor of pantothenic acid in Escherichia coli and functions as an endogenous metabolite and metabolic enzyme/protease. The incorporation of stable heavy isotopes, such as deuterium, into drug molecules is primarily used as tracers for quantitation during drug development. Deuteration also shows potential to influence the pharmacokinetic and metabolic profiles of drugs.
- Deuterium labeled compound
- Precursor of pantothenic acid in Escherichia coli
- Acts as an endogenous metabolite
- Functions as a metabolic enzyme/protease
- Used as a tracer in drug development
- Potential to affect pharmacokinetic and metabolic profiles of drugs
Cayman Chemical GK241, Purity: ≥98%, CAS: 1899930-93-8, 10 mg
An sPLA2 (Type IIA) inhibitor (IC50s = 0.143 and 0.068 µM for the human and mouse enzymes, respectively); inhibits IL-1β-induced production of PGE2 in isolated rat renal mesangial cells at 3 and 10 µM; inhibits SARS-CoV-2 Mpro (IC50 = 24 µM)
Cayman Chemical UNC569, Purity: ≥98%, CAS: 1350547-65-7, 10 mg
A TAM family kinase inhibitor (IC50s = 2.9, 37, and 48 nM for Mer, Axl, and Tyro3, respectively); antiproliferative against ALL cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively); inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively); decreases tumor burden by 47.8% relative to controls in human MYC transgenic zebrafish (4 μM); delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells (10 mg/kg)