GPR108 Inhibitors
Chemical inhibitors of GPR108 include a variety of compounds that interfere with signaling pathways essential for the protein's function. Wortmannin and LY294002 act as potent inhibitors of phosphoinositide 3-kinases (PI3K), key enzymes in cell signaling which indirectly affect GPR108 activity. By inhibiting PI3K, these chemicals reduce the phosphorylation of downstream targets, leading to the reduction of GPR108 signaling activity. Protein kinase C (PKC) inhibitors such as Go6983 and Bisindolylmaleimide I can also indirectly diminish GPR108 function by altering PKC-mediated signaling, which is potentially involved in regulating GPR108's activity. SB203580 specifically targets p38 MAP kinase, while PD98059 and U0126 are selective for inhibiting MEK1/2, both part of the MAPK signaling pathway. Inhibition of these kinases by SB203580, PD98059, and U0126 disrupts the stress response and MAPK/ERK pathway, respectively, leading to decreased activity of GPR108 due to reduced signal transduction efficiency.
Additionally, SP600125, a c-Jun N-terminal kinase (JNK) inhibitor, can decrease GPR108 signaling by impeding the function of JNK, which is part of the MAPK family and could be involved in GPR108-mediated pathways. Src family tyrosine kinases, which can be inhibited by PP2 and Dasatinib, also play a crucial role in several cell signaling pathways, and their inhibition can consequently lead to reduced GPR108 signaling. Furthermore, Staurosporine broadly inhibits protein kinases, which are critical for the signaling necessary for GPR108 function, thereby leading to a wide-ranging suppression of GPR108 activity. Lastly, Lestaurtinib targets JAK2 tyrosine kinase, part of the JAK-STAT signaling pathway, and by doing so, it can interfere with a pathway that regulates GPR108 signaling, thus functionally inhibiting GPR108.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a potent, irreversible inhibitor of phosphoinositide 3-kinases (PI3K), which are upstream regulators in pathways that could impact GPR108 signaling. By inhibiting PI3K, wortmannin can lead to a reduction in phosphorylation events that are critical for GPR108 function. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a specific inhibitor of PI3Ks, reducing the phosphorylation of downstream targets required for the proper functioning of GPR108. By disrupting PI3K activity, LY294002 can decrease the signaling cascade essential for GPR108's role in cellular processes. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
Go6983 is a potent inhibitor of protein kinase C (PKC) isoforms. As PKC is involved in a myriad of signaling pathways, including those that could regulate GPR108 activity, Go6983's inhibition of PKC can indirectly lead to a decrease in GPR108 signaling. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is another PKC inhibitor that can alter signaling pathways involving GPR108. By attenuating PKC-mediated signaling, this chemical can indirectly inhibit functional GPR108 signaling. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a specific inhibitor of p38 MAP kinase, which is involved in cellular stress responses. Inhibition of p38 MAP kinase can disrupt signaling pathways that potentially regulate GPR108 function, leading to a decrease in GPR108 activity. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 selectively inhibits MEK, which is upstream of ERK in the MAPK signaling pathway. Because GPR108 is involved in signaling pathways that interact with MAPK signaling, PD98059 can indirectly inhibit GPR108 by impairing ERK activation. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an inhibitor of c-Jun N-terminal kinase (JNK), which is part of the MAPK family. By inhibiting JNK, SP600125 can decrease the functional response of GPR108 that relies on this signaling pathway. | ||||||
PP 2 | 172889-27-9 | sc-202769 sc-202769A | 1 mg 5 mg | $92.00 $223.00 | 30 | |
PP2 is an inhibitor of Src family tyrosine kinases. Src kinases can affect numerous signaling pathways that may include GPR108-mediated signaling; thus, PP2 can indirectly decrease GPR108 activity. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Dasatinib is a broad-spectrum tyrosine kinase inhibitor with activity against Src family kinases. By inhibiting these kinases, Dasatinib can disrupt signaling pathways that are necessary for GPR108 activity. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a potent inhibitor of a wide range of protein kinases. As protein kinase-mediated signaling is important for GPR108 function, Staurosporine can lead to a broad inhibition of pathways necessary for GPR108 signaling. | ||||||