Cayman Chemical

Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC₅₀ = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

A podophyllotoxin derivative that causes dose-dependent single- and double-stranded breaks in DNA by inhibiting topoisomerase II; widely used in the treatment of various cancers.

A pan FGFR inhibitor (IC₅₀s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively); suppresses proliferation of cancer cells with wild-type FGFR3 overexpression and in an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3.

A peptidomimetic of the critical TNF-α recognition loop on TNF receptor I complex that prevents ligand interaction with the receptor; interferes with both activating receptor activator of NF-κB (RANK) and TNF-α’s recruitment and activation of osteoclasts, blocking bone...

A spiroketal antibiotic that inhibits EGF mitogenic activity, displays antiproliferative activity against human tumor cells, and demonstrates antifungal activity; inhibits bone resorption by inducing apoptosis in osteoclasts with an IC₅₀ value of 0.7 µM.

The EP4 receptor is one of four GPCRs that mediate the actions of prostaglandin E2 (PGE2). The diverse effects of PGE2 acting via EP4 receptors point to the need to identify novel agonists and antagonists, both to further elucidate the function of this receptor subtype and for use as therapeutics...

An intermediate in the HMG-CoA reductase pathway and used in the biosynthesis of terpenes, terpenoids, and sterols; also serves as a donor in post-translational isoprenylation of proteins.

A natural steroid sapogenin that has antioxidant and anti-inflammatory activities, is protective against metabolic and cardiovascular diseases, and can have immunomodulatory and estrogenic effects.

An inhibitor of PAD4 deimination activity (IC50 = 5.9 μM) that also inhibits PAD1 and PAD3 (IC50 = 0.8 and 6.2 μM, respectively); dose dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies in a CIA mouse model of inflammatory...

A major metabolite of magnolol that is 19-fold more potent than magnolol as a peripheral CB2 receptor agonist (EC₅₀ = 0.17 μM; Ki = 0.42 μM); also behaves as an antagonist at GPR55, a CB-related orphan receptor (KB = 13.3 μM).

An isopropyl ester of the free acid PG which corresponds to bimatoprost; a potent ocular hypotensive agent, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost, but with significantly more irritation.

An uncommon, naturally occurring PUFA, inhibits the binding of [3H]-LTB4 to porcine neutrophil membranes with a Ki value of 3 µM.

A farnesyl transferase inhibitor that blocks the post-translational lipid modification of oncogenic Ras isoforms H-Ras, N-Ras, and K-Ras (IC50s = 1.9, 2.8, and 5.2 nM, respectively) and Rheb (IC50 = 10-100 nM); demonstrates potent dose-dependent oral activity in an array of human tumor xenograft...

A mechanism-based inactivator of human CYP2B6 (Ki = 5.6 µM; IC₅₀ = 5.1 µM) with potent selectivity for CYP2B6 over other CYP450 isoforms.

Antigen: bovine PGIS amino acids 299-329 Host: rabbit Cross Reactivity: (+) bovine, ovine, and human PGIS; (−) rat PGIS Application(s): IP and WB PGIS catalyzes the isomerization of PGH2 to PGI2, a potent vasodilator and inhibitor platelet aggregation

Antigen: human S1P1 amino acids 241-253 Host: rabbit Cross Reactivity: (+) human, mouse, porcine, and rat S1P1 Application(s): ICC, IHC (formalin-fixed paraffin-embedded tissue), and WB S1P exerts its activity by binding to five distinct GPCRs, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and...

Binds the N-terminal domain of Hsp90, efficiently displacing geldanamycin from the ATP binding site (IC50 = 30 nM); inhibits the proliferation of several cancer cell lines (IC50 ~ 0.28 μM), promotes the degradation of Hsp90 client proteins, and has no effect on a variety of kinases.

A fungal metabolite that inhibits DGAT activity, preventing triacylglycerol formation (IC₅₀s = 17.5 and 2.8 µM in rat liver microsomes and Raji cells, respectively).

Source: Active recombinant N-terminal His-tag protein expressed in E. coli Mr: 43 kDa JMJD2A catalyzes the demethylation of trimethylated histone at lysine residues 9 and 36.

CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.

A positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s...

An orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC₅₀ values of 8, 60, 270, and 300 nM, respectively.

An internal standard for the quantification of PGF2α-EA by GC- or LC-MS.

A potent FAAH inhibitor, exhibiting Ki values of 0.094 and 0.2 nM for the human and rat enzymes, respectively.