2451070-32-7
Chemical Structure
L18I
- CAS No.: 2451070-32-7
- Formula:C47H51N11O8
- Molecular Weight:897.98
InChIKey: PQIHIELQKZACPK-LXJLEQQOSA-N
SMILES: O=C1C2=CC=CC(CCCOCCOCCOCCN3C=C(C(N4CCC[C@@H](N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C5N=CN=C8N)C4)=O)N=N3)=C2CN1C9C(NC(CC9)=O)=O
Biological Activity: L18I is a Bruton's tyrosine kinase (BTK) PROTAC degrader that targets wild-type and BTKC481, and recruits the cereblon E3 ligase to mediate proteasomal degradation. L18I regulates the BCR, TLR, FcγR and NLRP3 inflammasome signaling pathways, inhibits the phosphorylation of PLCγ-2, ERK1/2 and p38, and reduces the levels of B cell activation markers CD25, CD69 and CD86. L18I downregulates the NF-κB, TNF and TLR signaling pathways, reduces the production of pro-inflammatory cytokines, and decreases immune cell infiltration and immune complex deposition. L18I inhibits the proliferation of BTK-expressing lymphoma cells, induces tumor regression in xenograft models, and exhibits synergistic activity when combined with inhibitors of SYK, PI3K or Lyn. L18I can be used in research related to lupus, diffuse alveolar hemorrhage and B-cell lymphoma[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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L18I | 99.43% | L18I is a Bruton's tyrosine kinase (BTK) PROTAC degrader that targets wild-type and BTKC481, and recruits the cereblon E3 ligase to mediate proteasomal degradation. L18I regulates the BCR, TLR, FcγR and NLRP3 inflammasome signaling pathways, inhibits the phosphorylation of PLCγ-2, ERK1/2 and p38, and reduces the levels of B cell activation markers CD25, CD69 and CD86. L18I downregulates the NF-κB, TNF and TLR signaling pathways, reduces the production of pro-inflammatory cytokines, and decreases immune cell infiltration and immune complex deposition. L18I inhibits the proliferation of BTK-expressing lymphoma cells, induces tumor regression in xenograft models, and exhibits synergistic activity when combined with inhibitors of SYK, PI3K or Lyn. L18I can be used in research related to lupus, diffuse alveolar hemorrhage and B-cell lymphoma. | ||||||||||||||||||||
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- [1]. Zhu C, et al. PROTAC for Bruton's tyrosine kinase degradation alleviates inflammation in autoimmune diseases. Cell Discov. 2024 Aug 6;10(1):82. [Content Brief]
- [2]. Song Y, et al. Targeted protein degradation in autoimmune diseases: from mechanisms to therapeutic breakthroughs. Journal of autoimmunity. 2025 Sep;156:103475. [Content Brief]
- [3]. Arthur R, et al. Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors. Exploration of targeted anti-tumor therapy. 2020 Jun 29;1(3):131-152. [Content Brief]
- [4]. Wolska-Washer A, et al. Targeting Protein Degradation Pathways in Tumors: Focusing on their Role in Hematological Malignancies. Cancers. 2022 Aug 03;14(15):3778. [Content Brief]
- [5]. Sun Y, et al. Degradation of Bruton's tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas. Leukemia. 2019 Aug;33(8):2105-2110. [Content Brief]
Keywords
