Inflammation/Immunology

L-Glutamine-¹⁵N is the ¹⁵N-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways.

4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an oally ative estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC₅₀ values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.

Deltamethrin (Decamethrin) is an orally active synthetic pyrethroid insecticide. Deltamethrin induces oxidative stress and results in inflammation and apoptosis via inhibiting Nrf2/HO-1 pathway. Deltamethrin has an anticancer effect by inducing apoptosis. Deltamethrin can be used extensively in pest control.

Cortisone acetate (Cortisone 21-acetate), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acetate acts as an immunosuppressant and anti-inflammatory agent. Cortisone acetate can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.

IL-17A antagonist 1 is an interleukin-17A (IL-17A) antagonist with an IC₅₀ of 1.14 μM and a K_d of 0.66 μM. IL-17A antagonist 1 binds specifically and exclusively to the IL-17A homodimer at its central dimer interface pocket, induces a large conformational change that widens the pocket, and disrupts the IL-17A/IL-17RA interaction. IL-17A antagonist 1 does not bind to IL-17F or IL-17RA.

Xanthan gum interacts with gelatin (HY-Y1365) via hydrogen bonds, thereby increasing the viscosity and stability of the hydrogel while promoting cell growth and creating a microenvironment conducive to cell differentiation^[1][2]. Xanthan gum induces pro-inflammatory responses by increasing the levels of TNF-α, IL-6, and IL-10. Xanthan gum can be used for inflammation and immunology research.

Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC₅₀ of 248 nM and K_i of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety.

Zorifertinib (AZD3759) is a potent, orally active, BBB-penetrant, EGFR inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR^wt, EGFR^L858R, and EGFR^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research.

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

Rheb inhibitor NR1 is a Rheb inhibitor with an IC₅₀ of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity.
^{(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)}

Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research.

CORM-401 is an oxidant-sensitive CO-releasing molecule. CORM-401 induces NO increase in the regulation of endothelial calcium signalling. CORM-401 reduces TNF-α/CHX and H2O2-induced ROS production. CORM-401 uncouples mitochondrial respiration and inhibits glycolysis.

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC₅₀s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC₅₀s of 149 nM and 21.7 nM, respectively.

STL1267 is a potent and cross-the-blood-brain barrier REV-ERB agonist with a K_i value of 0.16 µM for REV-ERBα. STL1267 shows no cytotoxicity. STL1267 inhibits the gene expression of BMAL1.

WS6 is an IkB kinase and EBP1 inhibitor, with IC₅₀ values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats^[1][2][4].

Muromonab (Muromonab-CD3; OKT3) is a mouse monoclonal antibody targeting the CD3 antigen. Muromonab specifically binds to the CD3 antigen on the surface of human and higher primate T cells. Muromonab blocks the function of T cell receptors to recognize foreign antigens and inhibits T cell-mediated immune responses, including cell-mediated lymphocyte lysis and T cell proliferation responses. Muromonab can be used to study acute kidney, liver, heart and combined kidney-pancreas transplant rejection, and can also be used to study graft-versus-host disease in bone marrow transplant patients.

Obexelimab (XmAb5871) is a humanized anti-CD19 antibody. Obexelimab works by inhibiting B cell receptor (BCR) mediated calcium influx and promoting the phosphorylation of Fc γ receptor IIb (FcγRIIb), which reduces B cell activation and function, leading to B cell apoptosis. Obexelimab can be used in research for rheumatoid arthritis and systemic lupus erythematosus.

PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC₅₀ of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (K_d= 239 nM) than for Hsp90 (K_d= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase