3037514-38-5
Chemical Structure
BD-9136
- CAS No.: 3037514-38-5
- Formula:C44H44N10O5S
- Molecular Weight:824.95
InChIKey: WNTMFWJFGDGXOH-UHFFFAOYSA-N
SMILES: CC1=NN=C2COCC(C(CC3=CC=CC=C3)=C(S4)C#CC5=CN(N=C5)C6(CCN7CCN(CC7)C)CN(C8=C(C9=CC=C8)C(N(C9=O)C%10CCC(NC%10=O)=O)=O)C6)=C4N21
Biological Activity: BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
BD-9136 | 98.81% | BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Hu J, et al. Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity. Journal of medicinal chemistry. 2023 Jun 22;66(12):8222-8237. [Content Brief]
- [2]. Wang Y, et al. Novel, potent, and orally bioavailable LSD1 inhibitors induce fetal hemoglobin synthesis in a sickle cell disease mouse model. Blood. 2025 Jul 17;146(3):356-368. [Content Brief]
- [3]. Yu J, et al. Progestogen-driven B7-H4 contributes to onco-fetal immune tolerance. Cell. 2024 Aug 22;187(17):4713-4732.e19. [Content Brief]
