P5091 (P005091)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1062 | Check With Us |
| 500mg | $1805 | Check With Us |
| 1g | $2708 | Check With Us |
: Cat #: V1323 CAS #: 882257-11-6 Purity ≥ 98%
Description: P5091 (also called P5091; P-005091; P-5091; P005091) is a novel, potent, specific and selective inhibitor of ubiquitin-specific protease 7 (USP7) with potential anticancer activity.
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| Molecular Weight (MW) | 348.22 |
|---|---|
| Molecular Formula | C12H7Cl2NO3S2 |
| CAS No. | 882257-11-6 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 28 mg/mL (80.4 mM)rr |
| Water:<1 mg/mLrr | |
| Ethanol:<1 mg/mL | |
| Solubility In Vivo | 4% DMSO+30% PEG 400+ddH2O: 5mg/mL |
| Synonyms | P005091; P5091; P-005091; P-5091; P 005091; P 5091; 1-(5-((2,3-dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone |
| Protocol | In Vitro | P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53 |
|---|---|---|
| In Vivo | In animal tumor model studies, P005091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P005091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.8717 mL | 14.3587 mL | 28.7175 mL | 57.4350 mL |
| 5mM | 0.5743 mL | 2.8717 mL | 5.7435 mL | 11.4870 mL |
| 10mM | 0.2872 mL | 1.4359 mL | 2.8717 mL | 5.7435 mL |
| 20mM | 0.1436 mL | 0.7179 mL | 1.4359 mL | 2.8717 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.