SD-91  (Synonyms: STAT3 degrader-2)

SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a K_i of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506)^[1][2].

SD-91 (Compound 92) (0.2 μM, 1 μM, 30 nM, 100 nM, 300 nM; 3 h) decreased the level of total STAT3 protein in acute leukemia Molm-16 cells^[1].
In the BLI assays, SD-91 binds to STAT3 with a K_d value of 28 nM, while it displays a very weak affinity (K_d >10 μM) to all other STAT proteins (STAT1, STAT2, STAT4, STAT5A, STAT5B, and STAT6)^[2].
In the MOLM-16 acute leukemia, SU-DHL-1, and SUP-M2 lymphoma cell lines, SD-91 has IC₅₀ values of 0.17, 2.6, and 0.46 μM, respectively^[2].
SD-91 (1-10 μM; 4 h) effectively reduce the levels of STAT3 protein in a dose-dependent manner, with DC₅₀ values of 0.38 μM, 0.061μM, and 2.5 μM for MOLM-16, SU-DHL-1, and SUP-M2 cells, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SD-91 (Compound 92) (i.v.; 50 mg/kg; 6 h, 24 h, 48 h) decreased the level of total STAT3 protein and phosphorylated STAT3 (Y705) protein in acute leukemia Molm-16 tumors and SU-DHL-1 tumors in mice^[1].
SD-91 (i.v.; 25, 50 mg/kg; qw) shows antitumor activity against Molm-16 xenograft tumors in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1136.15

C₅₉H₆₂N₉O₁₃P

2497583-03-4

O=C(N1C[C@@H](C(N2[C@@](CC[C@H]2C(N[C@@H](CCC(N)=O)C(NC(C3=CC=CC=C3)C4=CC=CC=C4)=O)=O)([H])CC1)=O)NC(C5=CC6=CC(C(P(O)(O)=O)=O)=CC=C6N5)=O)CCCCCC#CC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7

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• [1]. Shaomeng Wang, et al. Small molecule degraders of stat3. Patent. WO2020198435A1.

  [2]. Zhou H, et al. SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression. ACS Med Chem Lett. 2021 May 10;12(6):996-1004.  [Content Brief]