Bioactive Small Molecules
Cayman Chemical ANTIBODY PIroxIcam 10g
A COX inhibitor and NSAID; inhibits TXB2 production from arachidonic acid in HEL human erythroleukemic cells (IC50 = 0.45 µM), as well as inhibits LPS-induced formation of PGF1α from arachidonic acid in Mono-Mac-6 cells (IC50 = 0.77 µM); reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays (IC50s = 240 and ~470 µM, respectively); reduces carrageenan-induced paw edema in rats at 1, 2.5, and 5 mg/kg
Cayman Chemical ANTIBODY PQ-10 10mg
A potent and selective inhibitor of phosphodiesterase type 10 (PDE10; Ki = 4 nM); has >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro; increases striatal cGMP and CREB phosphorylation in vivo; reduces scopolamine- and MK-801-induced memory deficits in rats; inhibits tumor cell growth with IC50 values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively
Cayman Chemical ANTIBODY PQR620 1mg
An mTOR inhibitor (Ki = 10.8 nM); selective for mTOR over PI3K p110α (Ki = 4.2 µM) and a panel of 456 other kinases at 10 µM; has antiproliferative activity against a panel of 66 cancer cell lines (mean IC50 = 919 nM); induces cell cycle arrest at the G1 phase in A2058 and SKOV3 cancer cells at 5 µM; decreases the number of seizures per week in a Tsc1GFAP conditional knockout mouse model of epilepsy at 100 mg/kg per day
Medchemexpress LLC NU074381b (compound 5b) | 98.5% | 396.91 | 100 MG
NU074381b is a potent S100A4 inhibitor (compound 5b) that disrupts the formation of the S100A4-NMII complex with an IC50 value of 0.48 μM. It inhibits cell proliferation and migration, and covalently inhibits S100A4 by reacting specifically with cysteine 81.
- Potent S100A4 inhibitor
- Disrupts S100A4-NMII complex formation
- Inhibits cell proliferation and migration
- Covalently inhibits S100A4 via cysteine 81
Medchemexpress LLC Bractoppin | 2290527-07-8 | 99.9% | 414.47 | C25H23FN4O | 100MG
Bractoppin is a small-molecule inhibitor that disrupts phosphopeptide recognition by the human BRCA1 tandem BRCT (tBRCT) domain. It preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response, reducing BRCA1 recruitment to DNA breaks, suppressing RAD51 assembly, and modulating damage-induced G2 arrest. In microscale thermophoresis assays it displaces a BACH1 phosphopeptide with a reported binding IC50 of 74 nM. Supplied as a high-purity research reagent for biochemical and cellular studies.
- High purity suitable for biochemical and cellular assays.
- Potent BRCA1 tBRCT inhibitor with nanomolar binding activity.
- Applicable to studies of DNA damage response and RAD51 recruitment.
- Provided as a weighed solid for solution preparation.
Medchemexpress LLC Edicotinib (JNJ-40346527) | 1142363-52-7 | 99.7% | 461.60 | 100 MG
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant, and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor. It exhibits lower inhibitory effects on KIT and FLT3. This compound limits microglial expansion, attenuates microglial proliferation, and reduces neurodegeneration in mice. It holds potential for research into Alzheimer's disease and rheumatoid arthritis.
- Potent and selective CSF-1R inhibitor
- Brain penetrant and orally active
- Limits microglial expansion
- Attenuates microglial proliferation
- Reduces neurodegeneration in mice
- Potential for Alzheimer's disease and rheumatoid arthritis research
- Available in solid form, white to off-white appearance
- Ships at room temperature
- Multiple solubility protocols for in vitro and in vivo studies
Medchemexpress LLC Migalastat hydrochloride (GR181413A) | 75172-81-5 | 99.7% | 199.63 | 100 MG
Migalastat hydrochloride (GR181413A) is an orally active α-galactosidase A molecular chaperone. It functions by binding to the active site of certain unstable mutant forms of α-galactosidase A, which facilitates their transport to the lysosome. Once in the acidic environment of the lysosome, Migalastat dissociates, allowing the mutant α-galactosidase A to exhibit biological activity.
- Orally active α-galactosidase A molecular chaperone
- IC50 value of 0.04 μM for human α-Gal A
- Facilitates transport of unstable mutant α-galactosidase A to the lysosome
- Enables mutant α-galactosidase A to exhibit biological activity
- Reduces Gb3 accumulation and lysosome volume in EHK cells mutated α-Gal A
- Increases α-Gal A activity in heart, kidney, spleen, and liver in transgenic mice
- Reduces lyso-Gb3 levels in kidney, heart, and skin in transgenic mice
Cayman Chemical HydrochlorothIazIde-3 3-d2 5mg
An internal standard for the quantification of hydrochlorothiazide by GC- or LC-MS
Medchemexpress LLC Iptacopan (hydrochloride) | 1646321-63-2 | 99.83% | 458.98 | 5 MG
Iptacopan hydrochloride is an effective, orally-active, and highly selective factor B inhibitor. It acts proximally in the complement cascade, preventing red blood cell destruction in paroxysmal nocturnal hemoglobinuria (PNH) and renal cell damage in immunoglobulin A nephropathy (IgAN) and complement 3 glomerulopathy (C3G).
- Effective, orally-active, and highly selective factor B inhibitor
- IC50 value of 10 nM and KD of 7.9 nM for factor B
- Prevents red blood cell destruction in PNH
- Prevents renal cell damage in IgAN and C3G
- Inhibits alternative complement pathway (AP)-induced membrane attack complex (MAC) formation
- Exhibits excellent selectivity over other proteases
- Used for studying complement-mediated diseases
![Medchemexpress LLC Pyrido[3,4-d]pyridazine-8-carbonitrile, 7-[[(1R,2S)-2-aminocyclohexyl]amino]-3,4-dihydro-5-[(3-methylphenyl)amino]-4-o | 2304654-43-9 | 99.8% | 389.45 | 5 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000364375-logo.png-250.jpg){kind=logo}
Medchemexpress LLC Pyrido[3,4-d]pyridazine-8-carbonitrile, 7-[[(1R,2S)-2-aminocyclohexyl]amino]-3,4-dihydro-5-[(3-methylphenyl)amino]-4-o | 2304654-43-9 | 99.8% | 389.45 | 5 MG
This product is a potent and orally active FER tyrosine kinase inhibitor, exhibiting anti-cancer activity with an IC50 of 0.49 nM. It is intended for research use only and not for patient use.
- Potent and orally active FER tyrosine kinase inhibitor
- IC50 of 0.49 nM
- Exhibits anti-cancer activity
- Intended for research use only
- Purity: 99.8%
- Molecular weight: 389.45
- Appearance: White to light yellow solid
- Soluble in DMSO at 200 mg/mL (513.54 mM)
- GI50 of 220 nM for growth inhibition in mouse mock transfected BA/F3 cells
- Long-term storage for powder at -20°C for 3 years, 4°C for 2 years
- Long-term storage in solvent at -80°C for 6 months, -20°C for 1 month
![Medchemexpress LLC Urea, N-butyl-N'-(10,11-dihydro-10-methyl-11-oxodibenzo[b,f]thiazepin-8-yl)- | 891509-95-8 | 98.0% | 355.45 | 5 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000364429-logo.png-250.jpg){kind=logo}
Medchemexpress LLC Urea, N-butyl-N'-(10,11-dihydro-10-methyl-11-oxodibenzo[b,f]thiazepin-8-yl)- | 891509-95-8 | 98.0% | 355.45 | 5 MG
SR-4995 is a highly effective and selective ligand for α-β-hydrolase domain-containing 5 (ABHD5). It facilitates the activation of adipose triglyceride lipase (ATGL) by displacing ABHD5 from its inhibitory regulators. SR-4995 directly interacts with ABHD5, promoting lipolysis in adipocytes and muscle tissues while circumventing PKA-dependent signaling pathways.
- Highly effective and selective ligand for α-β-hydrolase domain-containing 5 (ABHD5).
- Facilitates activation of adipose triglyceride lipase (ATGL).
- Displaces ABHD5 from inhibitory regulators, perilipin-1 (PLIN1) and PLIN5.
- Directly interacts with ABHD5, inhibiting its association with PLIN1.
- Promotes lipolysis in adipocytes and muscle tissues.
- Circumvents PKA-dependent signaling pathways.
Medchemexpress LLC Olcegepant (BIBN-4096) | 204697-65-4 | 99.6% | 869.65 | 5 MG
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor. It exhibits high affinity for the human CGRP receptor and can reverse CGRP-mediated vasodilation. Olcegepant has been studied for its role in inhibiting neurogenic vasodilation and reducing mechanical allodynia in animal models of migraine.
- Potent and selective non-peptide CGRP1 receptor antagonist
- IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP
- Exhibits higher affinity for human CGRP receptor than endogenous ligand CGRP
- Reverses CGRP-mediated vasodilation in human cerebral vessels
- Inhibits neurogenic vasodilation in animal models of migraine pathophysiology
- Reduces mechanical allodynia in CCI-ION rats
![Medchemexpress LLC Benzenesulfonamide, N-[2-[(1-amino-6-isoquinolinyl)oxy]-4-methylphenyl]-2-methoxy- | 2377379-39-8 | 99.9% | 435.50 | 5 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000364630-logo.png-250.jpg){kind=logo}
Medchemexpress LLC Benzenesulfonamide, N-[2-[(1-amino-6-isoquinolinyl)oxy]-4-methylphenyl]-2-methoxy- | 2377379-39-8 | 99.9% | 435.50 | 5 MG
MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC₅₀=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. It is inactive against MRGPRC11, which inhibits high voltage-activated Ca²⁺ currents and mitigates nociceptive transmission. This compound is useful for studying chronic pain, especially neuropathic pain.
- Highly potent MRGPRX1 agonist (EC₅₀=50 nM)
- Demonstrates greater than 50-fold selectivity for δ, μ, and κ opioid receptors
- Inactive against MRGPRC11
- Useful for studying chronic pain, particularly neuropathic pain
- Soluble in DMSO at 125 mg/mL
- Powder stable at -20°C for 3 years, 4°C for 2 years
- In solvent stable at -80°C for 6 months, -20°C for 1 month
Medchemexpress LLC Thalidomide-PEG4-COOH | 2828438-28-2 | 95.36% | 478.45 | 100 MG
Thalidomide-PEG4-COOH is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a linker used in PROTAC technology. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. This product is for research use only.
- Synthesized E3 ligase ligand-linker conjugate
- Incorporates a Thalidomide-based cereblon ligand
- Used in PROTAC technology for targeted protein degradation
- Exploits the intracellular ubiquitin-proteasome system
- Targets cereblon
- Appearance is oil
- Store at -20°C, protected from light
- Soluble in DMSO at 250 mg/mL
Medchemexpress LLC JNJ-10397049 | 708275-58-5 | 99.2% | 484.18 | 5 MG
JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. It is 600-fold selective for the OX2R over the OX1R. For research use only. In vivo, JNJ-10397049 (10-30 mg/kg) decreases the latency for persistent sleep and increased nonrapid eye movement and rapid eye movement sleep time. It also blocks ethanol self-administration, place preference, and reinstatement.
- Decreases the latency for persistent sleep and increases nonrapid eye movement and rapid eye movement sleep time.
- Blocks ethanol self-administration, place preference, and reinstatement.
- In vitro solubility: DMSO: 170 mg/mL (351.11 mM).
- In vivo suspended solution protocol: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline; solubility: 4.25 mg/mL (8.78 mM).
- In vivo clear solution protocol: 10% DMSO, 90% Corn Oil; solubility: ≥ 4.25 mg/mL (8.78 mM).