b-AP15 (NSC 687852)
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 500mg | $650 | Check With Us |
| 1g | $1050 | Check With Us |
| 5g | $3150 | Check With Us |
: Cat #: V1329 CAS #: 1009817-63-3 Purity ≥ 98%
Description: b-AP15 (formerly known as NSC687852; b-AP15; USP14 Inhibitor III; b-AP-15; NSC-687852) is a novel, potent and specific deubiquitinase (DUB) inhibitor of 19S proteasomes activity of Ub-AMC cleavage with potential antineoplastic activity.
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| Molecular Weight (MW) | 419.39 |
|---|---|
| Molecular Formula | C22H17N3O6 |
| CAS No. | 1009817-63-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 48 mg/mL (114.5 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 4% DMSO+corn oil: 1mg/mL |
| Synonyms | NSC687852, b-AP15; NSC-687852, b-AP15; NSC 687852, b-AP-15; USP14 Inhibitor III; UCHL5UCH37 Inhibitor II |
| Protocol | In Vitro | Purified 19S proteasomes (5 nM) are treated with indicated concentrations of b-AP15 and DUB activity is determined by detectionof Ub-AMC cleavage. The IC50 value (2.1±0.411 μM) is determined from log concentration curves in Graph Pad Prism using non linear regression analysis. b-AP15 as a previously unidentified class of proteasome inhibitor that abrogates the deubiquitinating activity of the 19S regulatory particle. b-AP15 inhibited the activity of two 19S regulatory-particle-associated deubiquitinases, ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14), resulting in accumulation of polyubiquitin. b-AP15 induced tumor cell apoptosis that is insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL |
|---|---|---|
| In Vivo | b-AP15 (2.5 mg/kg) inhibits tumor growth in syngenic mice models with less frequent administration schedules. We administered b-AP15 to C57BL/6J mice with Lewis lung carcinomas (LLCs) using a 2-d-on, 2-d-off schedule and to BALB/c mice with orthotopic breast carcinoma (4T1) using a 1-d-on, 3-d-off schedule. b-AP15 significantly inhibited tumor growth in both models, with T/C=0.16 (P≤0.01) for the C57BL/6J mice and T/C=0.25 (P≤0.001) for the BALB/c mice. A reduction in the number of pulmonary metastases also is observed in the group of mice with 4T1 breast carcinomas treated with b-AP15 |
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 | 2.3844 mL | 11.9221 mL | 23.8442 mL | 47.6883 mL |
| 5mM | 0.4769 mL | 2.3844 mL | 4.7688 mL | 9.5377 mL |
| 10mM | 0.2384 mL | 1.1922 mL | 2.3844 mL | 4.7688 mL |
| 20mM | 0.1192 mL | 0.5961 mL | 1.1922 mL | 2.3844 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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,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.