b-AP15

Cat.NO.:A619221 Purity:98%

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=CC2=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 MelJuSo UbG76V-YFP cells HeLa cells UMSCC1 cells monocyte-derived dendritic cells BFTC905 T24 T24/R RT4 MCF-7 T47D PK-15 cells 3D4/21 cells HNSCC cells SU-DHL-4 SU-DHL-2 RKO RKO-R HCT-15 HCT-15R HCT116 colon carcinoma cells KMBC cells HuCCT1 cells HAP1 BAP1 KO cells HAP1 WT cells IMR-32 LAN-6 HeLa cells HCT116 colon cancer cells	Concentration	Treated Time	Description	References

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 Mice Nude mice Nude mice Nude mice Nude mice Nude mice Nude mice Mice	Animal Model PRV infection model HNSCC tumor xenograft model SU-DHL-4 and SU-DHL-2 cell xenograft models CML xenograft model Colon cancer xenograft model RKO and RKO-R xenograft models NGP and SH-SY5Y xenograft models subcutaneous xenograft model	Administration	Dosage	Frequency	Description	References

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

References

[1]Lopez-Castejon G, Luheshi NM, et al. Deubiquitinases regulate the activity of caspase-1 and interleukin-1β secretion via assembly of the inflammasome. J Biol Chem. 2013 Jan 25;288(4):2721-33.

[2]D’Arcy P, Brnjic S, et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40.

[3]Wang X, D’Arcy P, Caulfield TR, Paulus A, Chitta K, Mohanty C, Gullbo J, Chanan-Khan A, Linder S. Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Chem Biol Drug Des. 2015 Nov;86(5):1036-48.

[4]Feng X, Holmlund T, Zheng C, Fadeel B. Proapoptotic effects of the novel proteasome inhibitor b-AP15 on multiple myeloma cells and natural killer cells. Exp Hematol. 2014 Mar;42(3):172-82.

[5]Tian Z, D’Arcy P, Wang X, Ray A, Tai YT, Hu Y, Carrasco RD, Richardson P, Linder S, Chauhan D, Anderson KC. A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood. 2014 Jan 30;123(5):706-16.

[6]D’Arcy P, Brnjic S, Olofsson MH, Fryknäs M, Lindsten K, De Cesare M, Perego P, Sadeghi B, Hassan M, Larsson R, Linder S. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40.

[7]D’Arcy P, Linder S. Proteasome deubiquitinases as novel targets for cancer therapy. Int J Biochem Cell Biol. 2012 Nov;44(11):1729-38.

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Isoform Comparison

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3′-Bromo-4′-fluoroacetanilide

PIPERAZINE， 1，4-BIS(2-CHLOROETHYL)-

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