Date published: 2026-5-30

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gremlin-2 Inhibitors

The chemical class of gremlin-2 inhibitors is a group of compounds that can indirectly influence the activity of gremlin-2, a protein implicated in various signaling pathways, including but not limited to TGF-beta, BMP, and possibly other pathways related to fibrosis and developmental processes. These chemicals typically work by inhibiting kinases or receptors within these pathways, thereby modulating the signaling cascade in a manner that results in reduced activity of gremlin-2. While gremlin-2's direct role and the mechanisms by which it acts are complex and not fully understood, the impact of these inhibitors is often assessed in terms of their capacity to alter the downstream effects of the pathways gremlin-2 is involved with.

The inhibitors outlined above are characterized by their ability to target specific receptors or kinases within the TGF-beta and BMP signaling pathways, which are central to gremlin-2's regulatory functions. The inhibitors include various types of small molecules, some of which have a more established background in affecting TGF-beta related signaling, such as TGF-beta receptor kinase inhibitors, ALK inhibitors, and COX-2 inhibitors. These inhibitors operate by binding to their targets and impeding the phosphorylation and subsequent signaling that would typically occur, which can, in turn, influence the modulation of gremlin-2 and its associated effects. While these compounds may not interact directly with gremlin-2, their effects on the signaling pathways provide a framework for understanding how they can indirectly reduce gremlin-2's activity, thereby influencing the biological processes in which gremlin-2 is a participant.

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Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Halofuginone

55837-20-2sc-507290
100 mg
$1775.00
(0)

Halofuginone is an inhibitor of the Smad3 phosphorylation, a downstream element of the TGF-beta pathway, which is potentially modulated by gremlin-2. By inhibiting Smad3 phosphorylation, halofuginone can reduce TGF-beta signaling, thus potentially decreasing the facilitative role of gremlin-2 in this pathway, which may lead to an overall reduction in gremlin-2 activity.

BML-275

866405-64-3sc-200689
sc-200689A
5 mg
25 mg
$96.00
$355.00
69
(1)

BML-275 inhibits BMP type I receptors ALK2, ALK3, and ALK6, which are part of the signaling pathways antagonized by gremlin-2. Inhibition of these receptors can lead to reduced BMP signaling, which may indirectly decrease the functional activity of gremlin-2 as it interacts with these pathways.

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

1062368-24-4sc-476297
5 mg
$240.00
(0)

This compound is a selective BMP signaling inhibitor, targeting ALK2 and ALK3 receptors. Gremlin-2 acts by binding BMPs, preventing their interaction with receptors. By inhibiting the receptors themselves, this compound could reduce the effectiveness of gremlin-2's antagonistic action on BMP signaling, thereby acting as an indirect inhibitor of gremlin-2.

SB 431542

301836-41-9sc-204265
sc-204265A
sc-204265B
1 mg
10 mg
25 mg
$82.00
$216.00
$416.00
48
(1)

SB-431542 selectively inhibits ALK4, ALK5, and ALK7, which are activin and TGF-beta type I receptors. Since gremlin-2 is involved in modulating TGF-beta signaling, inhibiting these receptors could potentially attenuate the impact of gremlin-2 on this pathway, effectively reducing its activity.

LY2157299

700874-72-2sc-391123
sc-391123A
5 mg
10 mg
$213.00
$359.00
3
(1)

LY2157299 is a TGF-beta receptor I kinase inhibitor. It blocks TGF-beta signaling, which is implicated in various cellular processes that gremlin-2 might modulate. By inhibiting this signaling pathway, LY2157299 could diminish gremlin-2's regulatory role, thus indirectly acting as an inhibitor.

EW-7197

1352608-82-2sc-507465
5 mg
$345.00
(0)

EW-7197 is an ALK5 inhibitor, targeting a key kinase in the TGF-beta signaling pathway. As gremlin-2 can modulate the TGF-beta pathway, inhibition of ALK5 can result in diminished gremlin-2 activity related to this pathway, effectively reducing its biological effects.

Pirfenidone

53179-13-8sc-203663
sc-203663A
10 mg
50 mg
$102.00
$416.00
6
(1)

Pirfenidone has shown to have anti-fibrotic properties by inhibiting TGF-beta synthesis and downregulating TGF-beta stimulated collagen production. Gremlin-2, a modulator of TGF-beta activity, may be indirectly inhibited by pirfenidone's action, leading to a decrease in its fibrotic activity.

LY2109761

700874-71-1sc-396262
sc-396262A
1 mg
5 mg
$89.00
$275.00
9
(1)

LY2109761 is a selective inhibitor of TGF-beta receptor I/II (ALK5/ALK4). It prevents TGF-beta-mediated Smad2/3 activation. Since gremlin-2 is implicated in TGF-beta signaling modulation, inhibiting TGF-beta receptors could negate the impact of gremlin-2 on this pathway, thus serving as an indirect inhibitor.

A 83-01

909910-43-6sc-203791
sc-203791A
10 mg
50 mg
$202.00
$811.00
16
(1)

A-83-01 is an inhibitor of ALK5, ALK4, and ALK7, reducing TGF-beta signaling. By inhibiting these receptors, it could potentially limit gremlin-2 activity, which is involved in the regulation of this pathway.

ALK5 Inhibitor II

446859-33-2sc-221234
sc-221234A
sc-221234B
sc-221234C
sc-221234D
sc-221234E
sc-221234F
1 mg
5 mg
10 mg
50 mg
100 mg
500 mg
1 g
$77.00
$153.00
$219.00
$663.00
$1248.00
$4382.00
$7850.00
8
(1)

ALK5 Inhibitor II is a selective inhibitor of ALK5, impeding the TGF-beta pathway. Gremlin-2, known to interact with components of the TGF-beta signaling cascade, may be indirectly inhibited by the action of RepSox, leading to reduced modulation of the pathway by gremlin-2.