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(+)-JQ1, BET Inhibitor

(+)-JQ1, BET Inhibitor

$109.00   $139.00
A potent and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4
Catalog No. Unit Price Qty
M60139-2 10 mM in DMSO (0.438 mL) $109.00
$139.00
M60139-2s 2 mg solid $109.00
$139.00

Details

Product Information
Molecular Weight: 456.99
Formula: C23H25ClN4O2S
Purity: ≥98%
CAS#: 1268524-70-4
Solubility: DMSO up to 100 mM
Chemical Name: (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

Biological Activity:

(+)-JQ1 is a potent and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4 with IC50 of ~0.018 μM, 0.033 μM, and 0.077 μM, respectively. It has > 100-fold selectivity over CREBBP (IC50 ~12.9 µM). (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively. It can induces squamous differentiation in NUT midline carcinoma (NMC) cell lines and inhibit tumor growth in NMC xenograft models in vivo. (+)-JQ1 also exhibits reversible contraceptive effects in germ cells from male mice.

How to Use:

In vitro:  (+)-JQ1 was used at 1-10 µM final concentration in various in vitro assays.

In vivo: (+)-JQ1 was administrated to mice by IP injection at 50 mg/kg once per day or by oral dosing at 30 mg/kg twice per day. 

Reference:

  1. 1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. (2010) Nature. 468(7327):1067-73. Zuber J, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. (2011) Nature. 478(7370):524-8.
  2. 2. Delmore JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. (2011) Cell. 146(6):904-17.
  3. 3. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. (2012) Cell. 150(4):673-84.
  4. 4. Ott CJ, et al. BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. (2012) Blood. 120(14):2843-52.
  5. 5. Lockwood WW, et al. Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins. (2012) Proc Natl Acad Sci USA. 109(47):19408-13.
  6. 6. Belkina AC, et al. BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses. (2013) J Immunol. 190(7):3670-8.
  7. 7. Lovén J, et al. Selective inhibition of tumor oncogenes by disruption of super-enhancers. (2013) Cell. 153(2):320-34. 

 



  JQ1_spec.pdf

  JQ1_MSDS.pdf



Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 456.99
Formula: C23H25ClN4O2S
Purity: ≥98%
CAS#: 1268524-70-4
Solubility: DMSO up to 100 mM
Chemical Name: (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

Biological Activity:

(+)-JQ1 is a potent and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4 with IC50 of ~0.018 μM, 0.033 μM, and 0.077 μM, respectively. It has > 100-fold selectivity over CREBBP (IC50 ~12.9 µM). (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively. It can induces squamous differentiation in NUT midline carcinoma (NMC) cell lines and inhibit tumor growth in NMC xenograft models in vivo. (+)-JQ1 also exhibits reversible contraceptive effects in germ cells from male mice.

How to Use:

In vitro:  (+)-JQ1 was used at 1-10 µM final concentration in various in vitro assays.

In vivo: (+)-JQ1 was administrated to mice by IP injection at 50 mg/kg once per day or by oral dosing at 30 mg/kg twice per day. 

Reference:

  1. 1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. (2010) Nature. 468(7327):1067-73. Zuber J, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. (2011) Nature. 478(7370):524-8.
  2. 2. Delmore JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. (2011) Cell. 146(6):904-17.
  3. 3. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. (2012) Cell. 150(4):673-84.
  4. 4. Ott CJ, et al. BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. (2012) Blood. 120(14):2843-52.
  5. 5. Lockwood WW, et al. Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins. (2012) Proc Natl Acad Sci USA. 109(47):19408-13.
  6. 6. Belkina AC, et al. BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses. (2013) J Immunol. 190(7):3670-8.
  7. 7. Lovén J, et al. Selective inhibition of tumor oncogenes by disruption of super-enhancers. (2013) Cell. 153(2):320-34. 

 



  JQ1_spec.pdf

  JQ1_MSDS.pdf



Products are for research use only. Not for human use.

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