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Chemical Structure : Tilpisertib
Catalog No.: PC-38374Not For Human Use, Lab Use Only.
Tilpisertib (GS-4875) is a potent, highly selective TPL2 kinase (COT, MAP3K8) inhibitor with IC50 of 1.3 nM, with no significant off-target binding activity.
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Tilpisertib (GS-4875) is a potent, highly selective TPL2 kinase (COT, MAP3K8) inhibitor with IC50 of 1.3 nM, with no significant off-target binding activity.
Tilpisertib (GS-4875) selectively inhibited LPS and TNFα-stimulated phosphorylation of TPL2, MEK, and ERK, with little to no inhibition of phosphorylated p38, JNK or p65.
Tilpisertib (GS-4875) similarly inhibited in the RNA production and secretion of TNFα, IL-1β, IL-6, and IL-8 following LPS stimulation in primary human monocytes.
GS-4875 inhibited the secretion of TNFα and IL-6 following LPS stimulation in monocyte-derived dendritic cells.
Tilpisertib (GS-4875) reduced TNFα-stimulated pERK with no effect on ERK activation downstream of EGF in A431 cells stimulated with either TNFα or EGF.
Tilpisertib (GS-4875) treatment showed dose and exposure dependent inhibition (IC50=667 nM) of LPS-stimulated TNFα production a rat LPS-TNFα model of acute inflammation.
| M.Wt | 593.132 | |
| Formula | C33H33ClN8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Matthew Warr, et al. Meeting: 2019 ACR/ARP Annual Meeting.
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