2761281-50-7
Chemical Structure
PROTAC(H-PGDS)-7
- CAS. Nr.: 2761281-50-7
- Formula:C40H38N8O7
- Molecular Weight:742.78
IUPAC Name: N-(4-(4-(4-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)piperazine-1-carbonyl)piperidin-1-yl)phenyl)-2-phenoxypyrimidine-5-carboxamide
InChIKey: KQNXUQJGOJWQGL-UHFFFAOYSA-N
SMILES: O=C(C1CCN(C2=CC=C(NC(C3=CN=C(OC4=CC=CC=C4)N=C3)=O)C=C2)CC1)N5CCN(C6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)CC5
Biological Activity: PROTAC (H-PGDS)-7 is a selective, linker-free H-PGDS PROTAC degrader with a DC50 of 17.3 pM. PROTAC (H-PGDS)-7 binds to CRBN and forms a ternary complex with H-PGDS, inducing the degradation of H-PGDS via the ubiquitin-proteasome system through polyubiquitination and proteasomal degradation processes. PROTAC (H-PGDS)-7 inhibits the upregulated expression of TNFα, IL-1β, TGFβ1 and CD11b in mice with cardiac hypertrophy models. PROTAC (H-PGDS)-7 can be used in studies related to Duchenne muscular dystrophy and allergic diseases[1][2][3].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
PROTAC(H-PGDS)-7 | 99.42% | PROTAC (H-PGDS)-7 is a selective, linker-free H-PGDS PROTAC degrader with a DC50 of 17.3 pM. PROTAC (H-PGDS)-7 binds to CRBN and forms a ternary complex with H-PGDS, inducing the degradation of H-PGDS via the ubiquitin-proteasome system through polyubiquitination and proteasomal degradation processes. PROTAC (H-PGDS)-7 inhibits the upregulated expression of TNFα, IL-1β, TGFβ1 and CD11b in mice with cardiac hypertrophy models. PROTAC (H-PGDS)-7 can be used in studies related to Duchenne muscular dystrophy and allergic diseases. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Yokoo H, et al. Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design. Journal of medicinal chemistry. 2021 Nov 11;64(21):15868-15882. [Content Brief]
- [2]. Osawa H, et al. Optimizing linker rigidity to improve intracellular behavior of PROTACs targeting hematopoietic prostaglandin D synthase. RSC medicinal chemistry. 2025 Sep 02;16(10):4721-30.
- [3]. Murakami Y, et al. Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D synthase. RSC medicinal chemistry. 2022 Dec 14;13(12):1495-1503.
