BMP2 Activators
BMP2 Activators are a collection of chemical compounds that facilitate the enhancement of BMP2's functional activity by influencing various cellular signaling pathways. Dorsomorphin, LDN-193189, DMH1, LDN-214117, ML347, and K02288 are all inhibitors of BMP type I receptors such as ALK2, ALK3, and ALK6, which normally act to phosphorylate SMAD proteins, leading to the suppression of BMP2 signaling. By inhibiting these receptors, these compounds prevent the normal inhibition of BMP2, effectively enhancing the functional activity of BMP2 through derepression. This mechanism is critical for processes such as bone development and repair, where BMP2 plays a significant role. Additionally, SB-431542 and A83-01, by inhibiting other members of the TGF-β superfamily receptors, particularly ALK4, ALK5, and ALK7, reduce the competitive inhibition from the TGF-β pathway, which can indirectly lead to an increase in BMP2 activity, further promoting its osteogenic effects.
Furthermore, Forskolin, by increasing cAMP levels, indirectly augments BMP2 function by stimulating protein kinase A (PKA), which can phosphorylate substrates that enhance BMP2 signaling pathways, particularly those involved in gene expression. Similarly, PTH (1-34) activates the cAMP/PKA signaling cascade, potentially increasing the expression of BMP2 and its receptors, thereby amplifying the effects of BMP2 on bone formation. Lithium chloride, through its inhibition of GSK-3β, leads to the accumulation of β-catenin, which synergizes with BMP2 signaling in osteoblast differentiation. Magnesium ascorbyl phosphate, a derivative of vitamin C, is believed to upregulate BMP2 expression, thus contributing to the enhancement of BMP2 signaling in bone regeneration. Collectively, these BMP2 Activators play a crucial role in modulating diverse signaling pathways that converge to elevate the functional activity of BMP2, a key protein in skeletal development and repair.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Dorsomorphin dihydrochloride | 1219168-18-9 | sc-361173 sc-361173A | 10 mg 50 mg | $186.00 $751.00 | 28 | |
Dorsomorphin is a potent, selective, and reversible inhibitor of BMP type I receptors ALK2, ALK3, and ALK6, which normally phosphorylate SMAD proteins leading to BMP2 signaling inhibition. When dorsomorphin inhibits these receptors, it prevents the inhibition of BMP2, thereby enhancing BMP2 activity through derepression. | ||||||
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 1062368-24-4 | sc-476297 | 5 mg | $240.00 | ||
LDN-193189 is a selective ALK2 and ALK3 inhibitor similar to dorsomorphin but with improved potency and selectivity. By inhibiting these receptors, it blocks the phosphorylation of SMAD1/5/8, derepressing the BMP2 signaling pathway and thus enhancing BMP2-mediated biological processes. | ||||||
DMH-1 | 1206711-16-1 | sc-361171 sc-361171B sc-361171A sc-361171C | 10 mg 25 mg 50 mg 100 mg | $213.00 $318.00 $632.00 $1047.00 | 2 | |
DMH1 is another selective BMP receptor inhibitor that specifically targets ALK2, ALK3, and ALK6. By inhibiting the BMP type I receptors, DMH1 leads to increased BMP2 signaling activities by preventing the negative feedback loop that would otherwise inhibit BMP2 functions. | ||||||
LDN-214117 | 1627503-67-6 | sc-507451 | 5 mg | $165.00 | ||
LDN-214117 is a potent and selective inhibitor of the BMP type I receptor ALK2. The inhibition of ALK2 by LDN-214117 results in the upregulation of BMP2 signaling due to the reduction of the receptor-mediated blocking of BMP2 signaling pathways. | ||||||
LDN 193719 | 1062368-49-3 | sc-489383 | 10 mg | $189.00 | ||
LDN 193719 is a selective and potent inhibitor of ALK1 and ALK2, which are BMP type I receptors. By blocking the activity of these receptors, ML347 enhances BMP2 signaling by preventing the phosphorylation and activation of SMAD proteins that would typically inhibit BMP2 activity. | ||||||
K02288 | 1431985-92-0 | sc-488981 | 5 mg | $330.00 | ||
K02288 is a potent and selective inhibitor of ALK2, ALK3, and ALK6. The inhibition of these receptors promotes BMP2 signaling by preventing the SMAD-dependent negative feedback mechanism that usually downregulates BMP2 activity. | ||||||
SB 431542 | 301836-41-9 | sc-204265 sc-204265A sc-204265B | 1 mg 10 mg 25 mg | $82.00 $216.00 $416.00 | 48 | |
SB-431542 is an inhibitor of the TGF-β superfamily type I receptors ALK4, ALK5, and ALK7, but it is also known to influence BMP signaling indirectly. By inhibiting these receptors, SB-431542 can enhance BMP2 signaling by reducing the competitive inhibition from TGF-β pathways that might otherwise modulate BMP2 functions. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $202.00 $811.00 | 16 | |
A83-01 is a selective inhibitor of ALK5, ALK4, and ALK7, which are part of the TGF-β receptor family. This compound indirectly enhances BMP2 signaling by decreasing the competitive inhibition from TGF-β signaling, thereby allowing BMP2 pathways to be more active. | ||||||
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 works by activating adenylyl cyclase, which increases intracellular cAMP levels and activates PKA. This activation can lead to phosphorylation events that enhance BMP2 signaling by promoting the expression of BMP2-responsive genes and proteins. | ||||||
Parathyroid hormone fragment (1-34) | 52232-67-4 | sc-487943 | 100 µg | $185.00 | ||
Parathyroid hormone fragment (PTH 1-34) engages the PTH1 receptor, leading to cAMP/PKA pathway activation, which may enhance BMP2 signaling by increasing the expression of BMP2 and its receptors, subsequently promoting BMP2-mediated osteogenic differentiation. | ||||||