LMBR1 Inhibitors
LMBR1 inhibitors encompass a range of chemical compounds that target various components of the Hedgehog signaling pathway, which is intimately connected to the functional activity of LMBR1. Cyclopamine and Jervine, both steroidal alkaloids, accomplish this task by binding to and inhibiting the activity of the SMO receptor, a critical component for the transduction of the Shh signal that normally leads to the activation of GLI transcription factors downstream of LMBR1. Similarly, Vismodegib and Taladegib, along with other small molecule inhibitors like Saridegib and PF-04449913, function as antagonists of the SMO receptor, effectively shutting down the Hedgehog signal cascade that would otherwise culminate in the functional activity of LMBR1. Itraconazole, although primarily an antifungal agent, also exhibits activity against SMO, showcasing the potential for drugs with primary indications outside of Hedgehog pathway modulation to inadvertently influence LMBR1's activity.
While SMO receptor antagonists form the backbone of LMBR1 inhibition, other compounds like GANT61 and Robotnikinin target different nodes within the Hedgehog pathway. GANT61 disrupts the pathway by inhibiting the transcriptional activity of GLI1 and GLI2, which would normally be activated by Hedgehog signaling and subsequently regulate the activity of LMBR1. Robotnikinin takes a more upstream approach, directly binding to and inhibiting Shh protein, thus preventing the initial activation of the receptor complex including LMBR1. The collective action of these inhibitors demonstrates a concerted effort to dampen the Hedgehog signaling pathway at multiple junctures, thereby indirectly reducing the functional activity of LMBR1, a protein involved in the regulation of limb development.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cyclopamine | 4449-51-8 | sc-200929 sc-200929A | 1 mg 5 mg | $92.00 $204.00 | 19 | |
Cyclopamine is a steroidal alkaloid inhibitor of the Hedgehog signaling pathway, which acts by binding to and inhibiting the Smoothened (SMO) receptor. Inhibition of SMO prevents the activation of the GLI family of transcription factors, which are downstream of LMBR1 in the Shh pathway. As LMBR1 is implicated in the Sonic hedgehog (Shh) pathway, Cyclopamine can indirectly decrease the functional activity of LMBR1 by preventing Shh signal transduction. | ||||||
Vismodegib | 879085-55-9 | sc-396759 sc-396759A | 10 mg 25 mg | $80.00 $96.00 | 1 | |
Vismodegib is a small molecule inhibitor of the SMO receptor in the Hedgehog signaling pathway. By binding to SMO, it prevents the activation of downstream Hedgehog target genes by the GLI transcription factors, thereby reducing the functional activity of LMBR1 by stopping the Shh pathway signaling. | ||||||
GANT61 | 500579-04-4 | sc-202630 sc-202630A sc-202630B | 1 mg 5 mg 10 mg | $63.00 $128.00 $200.00 | 6 | |
GANT61 is a GLI antagonist that inhibits the transcriptional activity of GLI1 and GLI2 in the Hedgehog signaling pathway. By preventing the transcription of Hedgehog target genes, GANT61 reduces the functional activity of LMBR1 indirectly, as it is part of the pathway regulating limb development. | ||||||
Robotnikinin | 1132653-79-2 | sc-396554 | 1 mg | $650.00 | 1 | |
Robotnikinin is a small molecule that blocks the Hedgehog signaling pathway by directly binding to and inhibiting Sonic Hedgehog (Shh) protein. By preventing Shh from activating its receptor complex including LMBR1, Robotnikinin can indirectly lead to the decreased functional activity of LMBR1. | ||||||
Jervine | 469-59-0 | sc-200934 sc-200934A | 1 mg 5 mg | $66.00 $240.00 | 1 | |
Jervine is a naturally occurring steroidal alkaloid that acts similarly to Cyclopamine, inhibiting the Hedgehog signaling pathway at the level of the SMO receptor. This will result in an indirect inhibition of LMBR1 function by preventing the normal activation of the Hedgehog signaling cascade. | ||||||
SANT-1 | 304909-07-7 | sc-203253 | 5 mg | $132.00 | 5 | |
SANT-1 is a potent antagonist of SMO and acts to inhibit Hedgehog signaling. Its inhibition of SMO leads to a decrease in GLI-mediated transcription of target genes, which indirectly affects the functional activity of LMBR1 by impeding the Shh pathway. | ||||||
Itraconazole | 84625-61-6 | sc-205724 sc-205724A | 50 mg 100 mg | $76.00 $139.00 | 23 | |
Itraconazole, an antifungal agent, has been found to exert off-target effects by inhibiting SMO and, consequently, the Hedgehog signaling pathway. This inhibition can indirectly reduce the functional activity of LMBR1 by preventing activation of the pathway. | ||||||
Saridegib | 1037210-93-7 | sc-507351 | 5 mg | $3500.00 | ||
Saridegib is another SMO antagonist that inhibits the Hedgehog signaling pathway, leading to a reduction in the activity of GLI transcription factors and an indirect decrease in LMBR1 activity by cutting off the signaling through the Shh pathway. | ||||||
Glasdegib | 1095173-27-5 | sc-507353 | 5 mg | $165.00 | ||
PF-04449913 is a selective inhibitor of the SMO receptor, blocking Hedgehog signaling. By doing so, it indirectly diminishes the functional activity of LMBR1 by interrupting the normal Hedgehog signaling that involves LMBR1. | ||||||