| Bioactivity | PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3. | ||||||||||||
| Invitro | PYR-41 increases total sumoylation in cells in addition to blocking ubiquitylation. PYR-41 attenuates cytokine-mediated nuclear factor-κB activation. PYR-41 also prevents the downstream ubiquitylation and proteasomal degradation of IκBα. Furthermore, PYR-41 inhibits degradation of p53 and activates the transcriptional activity of this tumor suppressor[1]. PYR-41 (50 μM) promotes accumulation of ubiquitinated proteins. PYR-41 causes a concentration-dependent (10-50 μM) decline in DUB activity in Z138 cells after 4 h. PYR-41 potently inhibits USP5 DUB activity, even at the lowest concentration (10 μM). PYR-41 potently (10-50 μM) inhibits the activity of various DUBs, determined to represent USP9x, USP5, USP14, UCH37 and UCH-L3. Co-treatment of Z138 cells with DTT and PYR-41 completely abolishes the accumulation of ubiquitinated proteins[2]. | ||||||||||||
| Name | PYR-41 | ||||||||||||
| CAS | 418805-02-4 | ||||||||||||
| Formula | C17H13N3O7 | ||||||||||||
| Molar Mass | 371.30 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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PYR-41
CAS: 418805-02-4 F: C17H13N3O7 W: 371.30
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with litt
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