662107

UbcH13 Inhibitor, NSC697923

The UbcH13 Inhibitor, NSC697923 controls the biological activity of UbcH13. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Sinónimos: UbcH13 Inhibitor, NSC697923, NSC697923, UBE2N Inhibitor, Ubiquitin-Conjugating Enzyme E2 N Inhibitor, 2-Nitro-5-tosylfuran, Ubc13 Inhibitor
• Fórmula empírica (notación de Hill): C₁₁H₉NO₅S
• Número de CAS: 343351-67-7
• Peso molecular: 267.26
• Número MDL: MFCD01925132
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: O=S(C1=CC=C(O1)[N+]([O-])=O)(C2=CC=C(C)C=C2)=O
• InChI: 1S/C11H9NO5S/c1-8-2-4-9(5-3-8)18(15,16)11-7-6-10(17-11)12(13)14/h2-7H,1H3
• Clave InChI: GAUHIPWCDXOLCZ-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable nitro-tosylfuran compound that selectively inhibits the E2 Ubiquitin-conjugating enzyme Ubc13- (Cat. No. 662103), but not UbcH5c-, catalyzed K63-linked polyUb chain formation by preventing Ubc13-Ub thioester bond formation. Effectively inhibits Ubc13-Uev1A (UBE2V1) E2 complex-mediated NF-κB activation (Effective Conc. = 2 µM in HEK293T, MEF, RAW264.7, and SUDHL-6 cultures), Ubc13-Mms2 (UBEV2) E2 complex-mediated DNA DSB (double-strand break) repair activation (Effective Conc. = 1 µM in U2OS cells), as well as Ubc13-dependent p53 nuclear export (Effective Conc.1 to 2 µM in OCI-Ly10 cells), but not Ubc13-independent NF-κB activation following TNF-α receptor stimulation. The combined NF-κB and p53 activation via Ubc13 inhibition is shown to be particularly effective against the proliferation of ABC (Activated B-cell-like; OCI-Ly3, OCI-Ly10) and GCB (Germinal center B-cell-like; OCI-Ly7, SUDHL-6) DLBCL (Diffuse Large B-Cell Lymphoma) lines, as well as primary DLBCL cultures, via apoptosis induction (Effective Conc.1 to 2 µM).

A cell-permeable nitrofuran compound that selectively inhibits the E2 Ubiquitin-conjugating enzyme Ubc13- (Cat. No. 438075), but not UbcH5c-, catalyzed K63-linked polyUb chain formation by preventing Ubc13-Ub thioester bond formation. Effectively inhibits Ubc13-Uev1A (UBE2V1) E2 complex-mediated NF-κB activation, Ubc13-Mms2 (UBEV2) E2 complex-mediated DNA DSB (double-strand break) repair activation, as well as Ubc13-dependent p53 nuclear export in cultures (1 to 2 µM). The combined NF-κB inhibition and p53 activation via Ubc13 inhibition is shown to be particularly effective against the proliferation of ABC (Activated B-cell-like) and GCB (Germinal center B-cell-like) DLBCL (Diffuse Large B-Cell Lymphoma) cell lines and primary DLBCL cultures via apoptosis induction (1 to 2 µM).

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
Ubc13

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Pulvino, M., et al. 2012. Blood 1668.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3