Date published: 2026-4-1

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PAPP-A2 Inhibitors

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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Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Retinoic Acid, all trans

302-79-4sc-200898
sc-200898A
sc-200898B
sc-200898C
500 mg
5 g
10 g
100 g
$66.00
$325.00
$587.00
$1018.00
28
(1)

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

446-72-0sc-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
(1)

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

66575-29-9sc-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
(3)

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

50-02-2sc-29059
sc-29059B
sc-29059A
100 mg
1 g
5 g
$91.00
$139.00
$374.00
36
(1)

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

4478-93-7sc-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
(1)

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

989-51-5sc-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
(1)

Epigallocatechin Gallate could downregulate PAPP-A2 expression by inhibiting DNA methyltransferases, leading to hypomethylation and silencing of gene promoters driving PAPP-A2 expression.

Quercetin

117-39-5sc-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
(2)

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

700-06-1sc-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
(1)

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

7439-93-2sc-252954
50 g
$214.00
(0)

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)

89464-63-1sc-200755
sc-200755A
sc-200755B
sc-200755C
10 mg
50 mg
100 mg
500 mg
$84.00
$301.00
$374.00
$779.00
25
(2)

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.