PAPP-A2 inhibitors are a class of chemical compounds designed to target and inhibit the activity of pregnancy-associated plasma protein-A2 (PAPP-A2), a metalloproteinase that belongs to the pappalysin family. PAPP-A2 is primarily known for its role in modulating the bioavailability of insulin-like growth factor (IGF) by cleaving IGF-binding proteins, particularly IGFBP-5 and IGFBP-3. This cleavage releases bound IGF, increasing its availability to bind to the IGF receptor, which is involved in regulating various cellular processes such as growth and development. By inhibiting PAPP-A2, these compounds interfere with its ability to regulate IGF bioavailability, thereby altering the IGF signaling pathway and affecting downstream cellular responses.
The mechanism of action of PAPP-A2 inhibitors involves binding to the enzyme and preventing it from cleaving IGF-binding proteins, thus maintaining the IGF in its bound and inactive state. This disruption of PAPP-A2 activity provides researchers with an important tool for studying the regulation of the IGF system and its broader implications in cellular growth, differentiation, and metabolism. Inhibiting PAPP-A2 allows for a deeper exploration of how the enzyme influences IGF signaling and the control of IGF-related biological processes. By studying PAPP-A2 inhibitors, scientists gain insights into the molecular mechanisms that govern growth factor availability and their interactions with cellular receptors, helping to reveal the complex regulatory networks that modulate cell proliferation, growth, and tissue maintenance. This knowledge is crucial for understanding how enzymes like PAPP-A2 orchestrate key processes in cell biology and organismal development.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
Retinoic acid could downregulate PAPP-A2 by binding to retinoic acid receptors that interact with the PAPP-A2 gene promoter, leading to transcriptional repression. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
As a tyrosine kinase inhibitor, genistein could decrease PAPP-A2 expression by hindering the phosphorylation of proteins involved in the PAPP-A2 gene transcription machinery. | ||||||
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 might decrease PAPP-A2 expression by elevating cAMP levels, which in turn could activate protein kinase A, leading to the phosphorylation and inhibition of transcription factors critical for PAPP-A2 gene expression. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Dexamethasone could suppress PAPP-A2 expression through glucocorticoid receptor-mediated transrepression, where the activated receptor directly interferes with the transcription factors responsible for PAPP-A2 gene transcription. | ||||||
D,L-Sulforaphane | 4478-93-7 | sc-207495A sc-207495B sc-207495C sc-207495 sc-207495E sc-207495D | 5 mg 10 mg 25 mg 1 g 10 g 250 mg | $153.00 $292.00 $489.00 $1325.00 $8465.00 $933.00 | 22 | |
DL-Sulforaphane might reduce PAPP-A2 expression by inhibiting histone deacetylase, which would cause tighter chromatin conformation and decreased access of transcriptional machinery to the PAPP-A2 gene. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $43.00 $73.00 $126.00 $243.00 $530.00 $1259.00 | 11 | |
Epigallocatechin Gallate could downregulate PAPP-A2 expression by inhibiting DNA methyltransferases, leading to hypomethylation and silencing of gene promoters driving PAPP-A2 expression. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $110.00 $250.00 $936.00 $50.00 | 33 | |
Quercetin could inhibit PAPP-A2 expression by disrupting specific transcription factor binding, thereby preventing initiation of transcription of the PAPP-A2 gene. | ||||||
Indole-3-carbinol | 700-06-1 | sc-202662 sc-202662A sc-202662B sc-202662C sc-202662D | 1 g 5 g 100 g 250 g 1 kg | $39.00 $61.00 $146.00 $312.00 $1032.00 | 5 | |
As a modulator of estrogen metabolism, indole-3-carbinol could decrease PAPP-A2 expression by altering estrogen receptor-mediated transcriptional activity on the PAPP-A2 gene promoter. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium chloride might reduce PAPP-A2 expression by inhibiting GSK-3β, leading to the activation of transcription factors that repress PAPP-A2 gene transcription. | ||||||
Dimethyloxaloylglycine (DMOG) | 89464-63-1 | sc-200755 sc-200755A sc-200755B sc-200755C | 10 mg 50 mg 100 mg 500 mg | $84.00 $301.00 $374.00 $779.00 | 25 | |
DMOG could inhibit PAPP-A2 expression by stabilizing HIF-1α under normoxic conditions, which can then bind and repress hypoxia-response elements in the PAPP-A2 gene promoter. | ||||||