SMD-3236

• Target :

  Epigenetic Reader Domain|||PROTACs

• Related Pathways :

  PROTAC|||Chromatin/Epigenetic

• Bioactivity :

  SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl) methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.

• Smiles :

  O=C1N=C2C3(C=4C(N2C=5C1=C(Cl)C=CC5)=CC(=CC4)C6CCN(C[C@H]7CC[C@@H](CC7)C8=CN([C@H](C(=O)N9[C@H](C(N[C@@H](CN%10CCOCC%10)C%11=CC=C(C=C%11)C=%12SC=NC%12C)=O)C[C@@H](O)C9)C(C)(C)C)N=N8)CC6)CCCCC3

• Molecular Formula :

  C61H75ClN10O5S

• Molecular Weight :

  1095.83

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C

• CAS Number :

  3033586-31-8