RFX-B Inhibitors
Chemical inhibitors of the regulatory factor X-B (RFX-B) function primarily through indirect mechanisms, as RFX-B itself is not the direct target of these compounds. These chemicals disrupt signaling pathways that are upstream or integral to the transcriptional regulation activities of RFX-B, particularly its role in modulating the expression of Major Histocompatibility Complex class II (MHC-II) genes. Compounds such as Cyclosporin A, Ascomycin, Tacrolimus, Pimecrolimus, and Sotrastaurin act by inhibiting the enzyme calcineurin. Upon binding to their respective immunophilins (cyclophilins for Cyclosporin A and FKBP12 for the others), these molecules impair the dephosphorylation activity of calcineurin. This inhibition prevents the nuclear factor of activated T-cells (NFAT) from translocating to the nucleus and binding to the promoter regions of MHC-II genes, a step that RFX-B is known to be involved in. Consequently, RFX-B's ability to regulate the expression of these genes is diminished.
Other chemicals, such as Sirolimus, also known as Rapamycin, target a different pathway by binding to FKBP12 but their primary mode of action is through the inhibition of the mammalian target of rapamycin (mTOR). By curbing mTOR activity, Sirolimus interferes with a range of transcriptional programs that can indirectly affect RFX-B's role in gene expression. Additionally, the PKC inhibitors Rottlerin and Sotrastaurin can suppress NFAT activation by impairing upstream signaling, leading to a similar downregulation of RFX-B-mediated gene expression. Furthermore, compounds like Curcumin, Resveratrol, PDTC, Bay 11-7082, and MG-132 target the NF-κB pathway. These inhibitors restrict the activation and nuclear translocation of NF-κB, which, in turn, is essential for the full activation of certain MHC-II genes that are under RFX-B's regulatory scope. By inhibiting NF-κB, these compounds reduce the expression of MHC-II genes, thereby inhibiting RFX-B's functionality in this context. Overall, the collective action of these inhibitors results in a reduced functional capacity of RFX-B to regulate its target genes within the immune system.
SEE ALSO...
Items 1 to 10 of 11 total
Display:
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $63.00 $92.00 $250.00 $485.00 $1035.00 $2141.00 | 69 | |
Cyclosporin A binds to cyclophilins, inhibiting calcineurin, which subsequently inhibits the NFAT pathway. RFX-B is essential for MHC-II gene expression which is activated by the NFAT pathway in certain immune cells. Inhibition of NFAT therefore leads to reduced function of RFX-B in this context. | ||||||
Ascomycin | 104987-12-4 | sc-207303B sc-207303 sc-207303A | 1 mg 5 mg 25 mg | $37.00 $176.00 $322.00 | ||
Ascomycin, an FK506-related compound, binds to FKBP12, inhibiting calcineurin similarly to Cyclosporin A, and thus inhibits the NFAT pathway. As the NFAT pathway is involved in the activation of MHC-II genes, this would inhibit the functional role of RFX-B in regulating MHC-II expression. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Sirolimus binds to FKBP12 but instead of affecting calcineurin, it inhibits mTOR. Inhibition of mTOR can lead to reduced expression of genes regulated by RFX-B because mTOR signaling influences transcriptional programs in immune cells including those that activate MHC-II genes. | ||||||
Pimecrolimus | 137071-32-0 | sc-208172 | 1 mg | $140.00 | 2 | |
Pimecrolimus, similar to Tacrolimus and Ascomycin, binds to FKBP12 and inhibits the calcineurin-NFAT pathway. This inhibition reduces the expression of MHC-II genes, and thereby functionally inhibits the regulatory role of RFX-B associated with these genes. | ||||||
Rottlerin | 82-08-6 | sc-3550 sc-3550B sc-3550A sc-3550C sc-3550D sc-3550E | 10 mg 25 mg 50 mg 1 g 5 g 20 g | $84.00 $166.00 $302.00 $2091.00 $5212.00 $16657.00 | 51 | |
Rottlerin is known to inhibit PKC delta. Since PKC delta can influence NFAT activation, which is involved in the expression of MHC-II genes, the inhibition of PKC delta by Rottlerin can indirectly lead to reduced RFX-B function in MHC-II gene regulation. | ||||||
Sotrastaurin | 425637-18-9 | sc-474229 sc-474229A | 5 mg 10 mg | $300.00 $540.00 | ||
Sotrastaurin inhibits multiple isoforms of PKC, which are upstream of the NFAT pathway. By inhibiting PKC and subsequently NFAT, it would inhibit the functional activity of RFX-B related to MHC-II gene regulation. | ||||||
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 has been reported to inhibit NF-κB activation, which is necessary for the expression of multiple genes including MHC-II genes regulated by RFX-B. By inhibiting NF-κB, Curcumin indirectly inhibits the functional role of RFX-B. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol can inhibit NF-κB activation. Given that NF-κB is involved in the transcriptional activation of various immune-related genes, including those controlled by RFX-B, its inhibition by Resveratrol can indirectly inhibit RFX-B function. | ||||||
Pyrrolidinedithiocarbamic acid ammonium salt | 5108-96-3 | sc-203224 sc-203224A | 5 g 25 g | $33.00 $64.00 | 11 | |
PDTC is an NF-κB inhibitor. By inhibiting NF-κB, PDTC indirectly inhibits RFX-B function by reducing the expression of MHC-II genes which RFX-B is known to regulate. | ||||||
BAY 11-7082 | 19542-67-7 | sc-200615B sc-200615 sc-200615A | 5 mg 10 mg 50 mg | $62.00 $85.00 $356.00 | 155 | |
Bay 11-7082 is an inhibitor of IκBα phosphorylation, which leads to inhibition of NF-κB activation. This would indirectly inhibit RFX-B function by reducing the activity of MHC-II genes. | ||||||