SML2074

FX1

≥98% (HPLC)

• Synonym(e): (5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid, (Z)-3-(5-(5-Chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid
• Empirische Formel (Hill-System): C₁₄H₉ClN₂O₄S₂
• CAS-Nummer: 1426138-42-2
• Molekulargewicht: 368.82
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: red-brown
• storage temp.: 2-8°C
• SMILES string: S1\C(=C2\c3c(ccc(c3)Cl)NC\2=O)\C(=O)N(C1=S)CCC(=O)O
• InChI key: VISHSGZPGQKEFX-KHPPLWFESA-N

Beschreibung

Biochem/physiol Actions

FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).

Second generation 79-6 derived BCL6 inhibitor with improved efficacy against diffuse large B cell lymphoma (DLBCL) both in vitro and in vivo.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable