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Chemical Structure| 1009817-63-3 Chemical Structure| 1009817-63-3
Chemical Structure| 1009817-63-3

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CAS No.: 1009817-63-3

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b-AP15 is an inhibitor of the ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5) and ubiquitin-specific-processing protease 14 (USP14). In purified 19S proteasomes, b-AP15 can inhibit DUB activity with an IC50 of 2.1 μM.

Synonyms: NSC 687852

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Product Details of b-AP15

CAS No. :1009817-63-3
Formula : C22H17N3O6
M.W : 419.39
SMILES Code : O=C1/C(CN(C(C=C)=O)C/C1=C\C2=CC=C([N+]([O-])=O)C=C2)=C/C3=CC=C([N+]([O-])=O)C=C3
Synonyms :
NSC 687852
MDL No. :MFCD26142662
InChI Key :GFARQYQBWJLZMW-JYFOCSDGSA-N
Pubchem ID :5351435

Safety of b-AP15

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target

  • UCH

    UCHL5, IC50:2.1 μM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
MelJuSo UbG76V-YFP cells 1 μM 1-3 hours To study the effect of b-AP15 on proteasome function, it was found that b-AP15 inhibited proteasome function and led to cell death. PMC4241954
HeLa cells 10 μM 2 hours Immunoblot analysis showed that b-AP15 induced the formation of high molecular weight complexes with USP14. PMC7152998
UMSCC1 cells 250 nM 24 hours b-AP15 significantly inhibited the growth and colony formation capacity of UMSCC1 cells. PMC10154301
monocyte-derived dendritic cells 10 nM, 100 nM, 500 nM, 1000 nM 24 hours Comparative analysis of effects of bortezomib and b-AP15 on dendritic cell phenotype and function, finding that b-AP15 had no compromising effects on these DC features. PMC6538843
BFTC905 up to 2000 nM 24 hours induced ER stress and apoptosis PMC9421311
T24 up to 2000 nM 24 hours induced ER stress and apoptosis PMC9421311
T24/R up to 2000 nM 24 hours induced ER stress and apoptosis PMC9421311
RT4 up to 2000 nM 24 hours induced ER stress and apoptosis PMC9421311
MCF-7 0.5, 1, 2, 5 μM 24, 48, 72 h To evaluate the effect of b-AP15 on the growth of ER+ breast cancer cells, results showed that b-AP15 significantly inhibited cell viability. PMC6155249
T47D 0.5, 1, 2, 5 μM 24, 48, 72 h To evaluate the effect of b-AP15 on the growth of ER+ breast cancer cells, results showed that b-AP15 significantly inhibited cell viability. PMC6155249
PK-15 cells 0–1 μM 24–48 hours To evaluate the inhibitory effect of b-AP15 on PRV-GFP proliferation, results showed that b-AP15 significantly inhibited PRV-GFP proliferation. PMC9450976
3D4/21 cells 0–1 μM 24–48 hours To evaluate the inhibitory effect of b-AP15 on PRV-GFP proliferation, results showed that b-AP15 significantly inhibited PRV-GFP proliferation. PMC9450976
HNSCC cells 250 nM 48 hours b-AP15 significantly reduced the proliferation and survival of HNSCC cells and induced apoptosis. PMC10154301
SU-DHL-4 0.205 μM 48 hours b-AP15 inhibited the proliferation and induced apoptosis in GCB-DLBCL cells. PMC6836452
SU-DHL-2 0.296 μM 48 hours b-AP15 inhibited the proliferation and induced apoptosis in ABC-DLBCL cells. PMC6836452
RKO 1-5 μM 48 hours b-AP15 significantly reduced the viability of RKO cells, with an IC50 value of 1.649 μM. PMC10692219
RKO-R 1-5 μM 48 hours b-AP15 significantly reduced the viability of RKO-R cells, with an IC50 value of 0.987 μM. PMC10692219
HCT-15 1-5 μM 48 hours b-AP15 significantly reduced the viability of HCT-15 cells, with an IC50 value of 1.453 μM. PMC10692219
HCT-15R 1-5 μM 48 hours b-AP15 significantly reduced the viability of HCT-15R cells, with an IC50 value of 0.858 μM. PMC10692219
HCT116 colon carcinoma cells 1 μM 6 hours To study the effect of b-AP15 on gene expression in HCT116 cells, it was found that b-AP15 induced the expression of genes related to oxidative stress, ER stress, and heat shock. PMC4241954
KMBC cells 13 nM 72 hours Evaluate the sensitivity of b-AP15 in low BAP1 expressing cells, results showed increased sensitivity in KMBC cells with low BAP1 expression PMC5264287
HuCCT1 cells 1.9 μM 72 hours Evaluate the sensitivity of b-AP15 in high BAP1 expressing cells, results showed lower sensitivity in HuCCT1 cells with high BAP1 expression PMC5264287
HAP1 BAP1 KO cells 9 nM 72 hours Evaluate the sensitivity of b-AP15 in BAP1 knockout cells, results showed increased sensitivity in HAP1 BAP1 KO cells PMC5264287
HAP1 WT cells 38 nM 72 hours Evaluate the sensitivity of b-AP15 in wild-type cells, results showed lower sensitivity in HAP1 WT cells PMC5264287
IMR-32 107.8 nM (IC50) 72 hours Inhibits cell proliferation and induces apoptosis PMC6565366
LAN-6 127.8 nM (IC50) 72 hours Inhibits cell proliferation and induces apoptosis PMC6565366
HeLa cells 20 mM b-AP15 increased the levels of ubiquitinated proteins in cells and led to a 2- to 2.5-fold stimulation of proteasomal peptidase activity. PMC9231471
HCT116 colon cancer cells 1 μM Assess the cytotoxicity of b-AP15 on colon cancer cells PMC7770821

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice PRV infection model Intraperitoneal injection 8 mg/kg Every two days for 10 days To evaluate the protective effect of b-AP15 on PRV infection in vivo, results showed that b-AP15 significantly reduced the mortality of PRV-infected mice and inhibited PRV replication. PMC9450976
Nude mice HNSCC tumor xenograft model subcutaneous injection 5 mg/kg multiple times per week for 2 weeks b-AP15 as a monotherapy or in combination with radiation significantly delayed tumor growth and enhanced survival. PMC10154301
Nude mice SU-DHL-4 and SU-DHL-2 cell xenograft models Intraperitoneal injection 5 mg/kg/day Once daily for 11 days b-AP15 significantly inhibited the growth of GCB- and ABC-DLBCL xenograft models. PMC6836452
Nude mice CML xenograft model Intraperitoneal injection 5 mg/kg/day Once daily until the tumor volume reached 1500 mm3 b-AP15 significantly inhibited tumor growth in the CML xenograft model and reduced tumor volume and weight. PMC9460481
Nude mice Colon cancer xenograft model Intraperitoneal injection 100 mg/kg Daily Evaluate the antitumor activity of EF24 in colon cancer xenograft model PMC7770821
Nude mice RKO and RKO-R xenograft models Intraperitoneal injection 8 mg/kg/d Once daily, continuous treatment b-AP15 significantly suppressed the growth of RKO and RKO-R xenograft tumors without significantly affecting mouse body weight. PMC10692219
Nude mice NGP and SH-SY5Y xenograft models Intraperitoneal injection 5 mg/kg Once daily for two weeks Inhibits tumor growth and induces tumor cell apoptosis PMC6565366
Mice subcutaneous xenograft model intraperitoneal injection 7.5 mg/kg thrice a week for 4 weeks the combination of b-AP15 and cisplatin is superior to cisplatin monotherapy against UC in vivo PMC9421311

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL

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