CID5721353

SKU: orb1225385

Description

BCL6 inhibitor 79-6 (Compound 79-6) is the first-generation, specific BCL6 BTB domain inhibitor with IC50 of 200 uM, Kd of 129 uM; binds to a pocket in the lateral groove of the BCL6 BTB domain, specifically inhibits BCL6 but not other BTB-ZF proteins; disrupts BCL6/corepressor complexes and reactivates BCL6 target genes in vitro and in vivo, selectively kills BCL6-dependent DLBCL cells; suppresses human DLBCL xenografts in mice with favorable pharmacokinetics.

Key Properties

• CAS Number: 301356-95-6
• MW: 457.269
• Purity: >98% (HPLC)
• Formula: C₁₅H₉BrN₂O₆S₂
• SMILES: O=C(O)C(N(C/1=O)C(SC1=C2C(NC3=C/2C=C(Br)C=C3)=O)=S)CC(O)=O
• Target: Bcl-2
• Solubility: < 1 mg/ml refers to the product slightly soluble or insoluble

Bioactivity

• In Vivo:
  In order to test whether CID5721353 (Compound 79-6) can perform as an anti-lymphoma therapeutic agent In vivo, whether it can penetrate tumors after parenteral administration through a distal site is determined. For this purpose 107OCI-Ly7 cells are injected into the right flank of 10 SCID mice and allowed to form tumors. Once tumors reach ~1.5 grams, animals are injected IP with a single dose of 50 mg/kg of CID5721353 in 10% DMSO or vehicle (10% DMSO) and sacrificed at 0.5, 1, 1.5, 3, 6, 12 and 24 hours after CID5721353 administration. Blood and tumors are harvested. Quantitative HPLC/MS analysis of the serum shows that CID5721353 levels peak (to 55 μg/mL, which is equivalent to a 122 μM concentration) one hour after the IP injection. CID5721353 also reaches its highest peak (24.5 ng/mg) at the 1-hour time point in the tumors, and after a sharp decline in levels, decreases gradually over 24 hours.
• In Vitro:
  BCL6 is a member of the BTB/POZ family of transcription factors. CID5721353 (Compound 79-6) specifically inhibits BCL6 repressor activity. CID5721353 disrupts BCL6 transcriptional complexes and reactivates BCL6 target genes. CID5721353 can specifically kill primary human DLBCL cells. Fifteen of 19 BCL6-positive cases (79%) display greater than 25% loss of viability in response to CID5721353 at 125 or 250 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CID5721353 | CID-5721353 | CID 5721353 | BCL6 Inhibitor

Quick Database Links

Gene Symbol

Bcl-2