Date published: 2026-5-5

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gremlin-1 Inhibitors

The chemical class of gremlin-1 inhibitors constitutes a diverse spectrum of compounds, each designed with unique mechanisms to target the intricate TGF-β and BMP pathways. Kavain, an intriguing natural compound found in kava, stands out as an indirect inhibitor of gremlin-1. This compound operates by suppressing TGF-β signaling, providing valuable insights into the complex crosstalk between kava-derived compounds and cellular responses mediated by the TGF-β pathway. In contrast, direct inhibitors like LDN-193189 and RepSox play pivotal roles in selectively targeting BMP and TGF-β receptor signaling, respectively. By disrupting the downstream events associated with these pathways, these compounds effectively impede the upregulation of gremlin-1. The specificity of LDN-193189 and RepSox offers valuable tools for researchers delving into the regulatory mechanisms governing gremlin-1 within the context of BMP and TGF-β pathways. These inhibitors pave the way for a more nuanced understanding of how gremlin-1 fits into the broader landscape of cellular signaling.

Expanding the repertoire of direct inhibitors, SB-431542, LDN-214117, Galunisertib, GW788388, LY2157299, and SD-208 take center stage by specifically targeting the TGF-β pathway. These compounds exert their inhibitory effects by modulating gremlin-1 expression through the inhibition of TGF-β receptor activation. Each member of this chemical class contributes a unique perspective, unraveling the intricacies of TGF-β-mediated regulation of gremlin-1. SB-431542, for instance, may offer distinct mechanistic insights compared to the others, enriching the toolkit available for researchers aiming to decipher the role of gremlin-1 in diverse physiological and pathological contexts. In conclusion, the chemical class of gremlin-1 inhibitors presents a rich assortment of compounds, each with its distinct characteristics and mechanisms of action.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Kavain (±)

500-64-1sc-201077
sc-201077A
50 mg
250 mg
$72.00
$300.00
2
(0)

Kavain, a natural compound from kava, inhibits gremlin-1 indirectly by suppressing TGF-β signaling. By attenuating TGF-β1-induced Smad2/3 phosphorylation, Kavain modulates the TGF-β pathway, impacting gremlin-1 expression. This indirect inhibition provides insights into the crosstalk between Kavain and TGF-β signaling, offering a tool for investigating gremlin-1 regulation in the context of TGF-β-mediated cellular responses.

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

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

LDN-193189, a selective BMP type I receptor inhibitor, directly targets the BMP pathway, inhibiting gremlin-1 expression. By blocking BMP receptor signaling, LDN-193189 disrupts the downstream events leading to gremlin-1 upregulation. This direct inhibition provides a specific tool for studying the role of LDN-193189 in modulating gremlin-1 and its implications in BMP pathway regulation.

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)

RepSox, a selective TGF-β receptor I kinase inhibitor, directly targets the TGF-β signaling pathway, modulating gremlin-1 expression. By inhibiting TGF-β receptor activation, RepSox interferes with the downstream events leading to gremlin-1 upregulation. This direct inhibition offers a specific tool for investigating the regulatory mechanisms governing gremlin-1 in the context of TGF-β-mediated cellular responses.

LDN-214117

1627503-67-6sc-507451
5 mg
$165.00
(0)

LDN-214117, a selective BMP type I receptor inhibitor, directly targets the BMP pathway, inhibiting gremlin-1 expression. By blocking BMP receptor signaling, LDN-214117 disrupts the downstream events leading to gremlin-1 upregulation. This direct inhibition provides a specific tool for studying the role of LDN-214117 in modulating gremlin-1 and its implications in BMP pathway regulation.

LY2157299

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

LY2157299, a selective TGF-β receptor I kinase inhibitor, directly targets the TGF-β signaling pathway, modulating gremlin-1 expression. By inhibiting TGF-β receptor activation, LY2157299 interferes with the downstream events leading to gremlin-1 upregulation. This direct inhibition offers a specific tool for investigating the regulatory mechanisms governing gremlin-1 in the context of TGF-β-mediated cellular responses.

GW788388

452342-67-5sc-363544
sc-363544A
5 mg
25 mg
$95.00
$384.00
(0)

GW788388, a selective TGF-β receptor I kinase inhibitor, directly targets the TGF-β signaling pathway, influencing gremlin-1 expression. By inhibiting TGF-β receptor activation, GW788388 modulates the downstream events leading to gremlin-1 upregulation. This direct inhibition provides a specific tool for studying the regulatory mechanisms governing gremlin-1 in the context of TGF-β-mediated cellular responses.

TGF-β RI Kinase Inhibitor V

627536-09-8sc-203294
2 mg
$88.00
3
(1)

SD-208, a selective TGF-β receptor I kinase inhibitor, directly targets the TGF-β signaling pathway, influencing gremlin-1 expression. By inhibiting TGF-β receptor activation, SD-208 modulates the downstream events leading to gremlin-1 upregulation. This direct inhibition provides a specific tool for studying the regulatory mechanisms governing gremlin-1 in the context of TGF-β-mediated cellular responses.