CAS NO: | 418805-02-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 |
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzymeE1with anIC50of< 10 μM, with little activity at E2 and E3. |
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IC50& Target |
IC50:< 10 μM (E1) |
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体外研究 (In Vitro) |
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].
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分子量 |
371.30 |
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性状 |
Solid |
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Formula |
C17H13N3O7 |
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CAS 号 |
418805-02-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 46 mg/mL(123.89 mM) *"≥" means soluble, but saturation unknown.
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In Vivo:
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