GITRL Activators
GITRL Activators are a range of chemical compounds that bolster the activity of GITRL, a member of the tumor necrosis factor (TNF) receptor superfamily involved in the co-stimulation and proliferation of Tcells. Forskolin and Prostaglandin E2, through their elevation of intracellular cAMP, activate protein kinase A (PKA), which subsequently can phosphorylate and enhance the expression of GITRL, thereby amplifying its ability to engage with its receptor on T cells, leading to a robust immune response. Similarly, Brefeldin A, by disrupting the Golgi apparatus, may inadvertently enhance GITRL's presence on the cell surface, increasing its availability to interact with T cells. Phorbol 12-myristate 13-acetate (PMA) activates protein kinase C (PKC), a key regulator in the trafficking and expression of TNFR family proteins, thereby potentially increasing the functional activity of GITRL at the cell surface. Ionomycin, by raising intracellular calcium levels, leads to the activation of calcineurin, which then enhances the nuclear translocation of NFAT, a transcription factor that could upregulate GITRL expression and activity.
In addition to these, SB 216763, a glycogen synthase kinase-3 (GSK-3) inhibitor, stabilizes β-catenin, promoting Wnt signaling which has been implicated in the enhancement of GITRL expression. Resveratrol and Piperlongumine activate and increase the activity of NF-kB signaling, respectively, driving up the expression of GITRL and its subsequent role in immune cell co-stimulation. Curcumin, though typically an NF-kB inhibitor, may paradoxically promote GITRL's co-stimulatory role by modulating immune response balances. CP-690550, known as Tofacitinib, by inhibiting Janus kinase (JAK), may impact cytokine signaling and thus favor the co-stimulatory actions of GITRL. Zoledronic Acid, through its inhibition of farnesyl pyrophosphate synthase, may enhance GITRL's activity particularly in γδ T-cell activation and co-stimulation, due to the accumulation of isopentenyl pyrophosphate (IPP). Lastly, A-769662 activates AMP-activated protein kinase (AMPK), which can modulate immune responses, suggesting a potential upregulation of GITRL's expression and co-stimulatory function, highlighting the diverse yet convergent mechanisms by which these activators may enhance GITRL function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $78.00 $153.00 $740.00 $1413.00 $2091.00 | 73 | |
Forskolin directly stimulates adenylyl cyclase, increasing intracellular cAMP levels. Elevated cAMP activates PKA, which can then phosphorylate proteins involved in the TNFR pathway, enhancing GITRL's role in T-cell costimulation and the amplification of immune responses. | ||||||
PGE2 | 363-24-6 | sc-201225 sc-201225C sc-201225A sc-201225B | 1 mg 5 mg 10 mg 50 mg | $57.00 $159.00 $275.00 $678.00 | 37 | |
PGE2 interacts with its EP2/EP4 receptors, leading to an increase in intracellular cAMP. This activation of the cAMP-PKA signaling pathway can enhance the effectiveness of GITRL in T-cell activation through improved co-stimulatory signaling. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $31.00 $53.00 $124.00 $374.00 | 25 | |
Brefeldin A disrupts the structure and function of the Golgi apparatus, which can lead to an accumulation of GITRL in the ER, potentially increasing its trafficking to the cell surface where it can interact more effectively with its receptor on T-cells to stimulate immune responses. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA activates protein kinase C (PKC), which is known to regulate the trafficking and surface expression of various TNFR family proteins. By enhancing PKC activity, PMA can increase the functional activity of surface-expressed GITRL, promoting its co-stimulatory capacity. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin is a calcium ionophore that raises intracellular calcium levels, activating calcineurin. Activated calcineurin can dephosphorylate NFAT, leading to its nuclear translocation and the upregulation of proteins involved in immune responses, potentially enhancing GITRL activity. | ||||||
SB-216763 | 280744-09-4 | sc-200646 sc-200646A | 1 mg 5 mg | $71.00 $202.00 | 18 | |
SB-216763 is a GSK-3 inhibitor which leads to the stabilization and nuclear translocation of β-catenin. β-catenin can then enhance Wnt signaling, which has been implicated in the regulation of GITRL expression, thereby potentially increasing GITRL-mediated co-stimulation. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol activates SIRT1, which can deacetylate and activate transcription factors such as NF-kB. Activation of NF-kB can lead to the upregulation of co-stimulatory molecules including GITRL, thus enhancing its functional activity in T-cell costimulation. | ||||||
Piperlongumine | 20069-09-4 | sc-364128 | 10 mg | $107.00 | ||
Piperlongumine increases ROS levels, which can activate NF-kB signaling. Activation of NF-kB may lead to enhanced expression and activity of GITRL, contributing to its role in T-cell activation and the immune response. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Curcumin can inhibit NF-kB activation, leading to a modulation of immune responses. In the context of GITRL, this inhibition may shift the balance towards co-stimulatory signaling, potentially enhancing GITRL's activity in T-cell engagement. | ||||||
Zoledronic acid, anhydrous | 118072-93-8 | sc-364663 sc-364663A | 25 mg 100 mg | $92.00 $256.00 | 5 | |
Zoledronic Acid inhibits farnesyl pyrophosphate synthase, leading to the accumulation of isopentenyl pyrophosphate (IPP) and enhanced presentation of non-peptide antigens, potentially upregulating GITRL's activity in γδ T-cell activation and co-stimulation. | ||||||