MPP4 Activators
Chemical activators of MPP4 play a pivotal role in the modulation of its activity through different signaling pathways. Phorbol 12-myristate 13-acetate (PMA), for instance, directly activates Protein Kinase C (PKC), which can phosphorylate MPP4, enhancing its function in cellular signaling. Similarly, 1-Oleoyl-2-acetyl-sn-glycerol (OAG) mimics diacylglycerol (DAG) to activate PKC isoforms, which also phosphorylates MPP4. Ionomycin and Calcium ionophore A23187 both raise intracellular calcium levels, which can activate calmodulin-dependent protein kinase II (CaMKII). The activation of CaMKII can lead to the phosphorylation of MPP4. Furthermore, forskolin activates adenylyl cyclase, which increases cAMP levels and activates Protein Kinase A (PKA), leading to the phosphorylation and activation of MPP4.
Certain chemicals inhibit the dephosphorylation of MPP4, maintaining it in an active state. Okadaic acid and Calyculin A are inhibitors of protein phosphatases PP1 and PP2A, thus preserving the phosphorylated state of MPP4. Additionally, 8-Bromoadenosine 3',5'-cyclic monophosphate (8-Br-cAMP) and N6-Benzoyladenosine 3',5'-cyclic monophosphate (6-Bnz-cAMP) are cAMP analogs that activate PKA, which in turn activates MPP4. Thapsigargin disrupts calcium homeostasis by inhibiting the sarco/endoplasmic reticulum Ca²⁺-ATPase (SERCA), resulting in increased cytosolic calcium levels that can activate kinases such as CaMKII, subsequently leading to MPP4 activation. BIM (Bisindolylmaleimide I), on the other hand, inhibits PKC but can also induce a conformation that leads to basal activity of PKC, resulting in the activation of MPP4.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 directly activates Protein Kinase C (PKC) which can lead to the activation of MPP4 through phosphorylation as MPP4 is known to be a PKC substrate. This phosphorylation can enhance MPP4's function in cellular signaling. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
A23187 increases intracellular calcium levels, which can activate calmodulin-dependent protein kinase II (CaMKII). CaMKII activation can lead to the phosphorylation and functional activation of MPP4, as MPP4 has been identified as a potential CaMKII substrate. | ||||||
1-Oleoyl-2-acetyl-sn-glycerol (OAG) | 86390-77-4 | sc-200417 sc-200417A | 10 mg 50 mg | $119.00 $453.00 | 1 | |
OAG serves as a diacylglycerol analog, activating PKC isoforms. This activation of PKC can result in the phosphorylation and subsequent activation of MPP4, given PKC's role in downstream signaling. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin increases intracellular Ca²⁺ concentration, which can activate calcium-sensitive signaling pathways involving calmodulin and CaMKII, leading to the subsequent activation of MPP4 through phosphorylation. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Okadaic acid is an inhibitor of protein phosphatases PP1 and PP2A, preventing dephosphorylation of proteins. This indirect mechanism preserves the phosphorylation state of MPP4, maintaining its activated form. | ||||||
8-Bromo-cAMP | 76939-46-3 | sc-201564 sc-201564A | 10 mg 50 mg | $126.00 $328.00 | 30 | |
8-Br-cAMP is a cAMP analog that activates PKA. PKA can then phosphorylate and activate MPP4 in signal transduction related to vision as MPP4 is present in the retina and linked to photoreceptor function. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin inhibits the sarco/endoplasmic reticulum Ca²⁺-ATPase (SERCA), leading to increased cytosolic calcium levels, potentially activating CaMKII, which might then phosphorylate and activate MPP4. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Calyculin A is an inhibitor of protein phosphatases PP1 and PP2A. By inhibiting dephosphorylation, it can maintain MPP4 in a phosphorylated and activated state, thereby sustaining its functional activity. | ||||||
1,2-Dioctanoyl-sn-glycerol | 60514-48-9 | sc-202397 sc-202397A | 10 mg 50 mg | $47.00 $254.00 | 2 | |
DAG directly activates certain PKC isoforms. Through PKC activation, MPP4 can be phosphorylated and activated, as it is a known downstream target of PKC in signal transduction pathways. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
BIM is a PKC inhibitor, but paradoxically, it can act as an activator of PKC substrates by inducing a pseudo-substrate PKC conformation that leads to a basal level of PKC activity. This can result in the activation of MPP4 through phosphorylation. | ||||||