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SCR7, NHEJ inhibitor

SCR7, NHEJ inhibitor

$129.00
A potent and selective inhibitor of non-homologous end joining (NHEJ).
Catalog No. Unit Price Qty
M60082-2s 2 mg solid $129.00
M60082-2 10 mM DMSO (0.598 mL) $129.00

Details

Product Information
Molecular Weight: 334.39
Formula: C18H14N4OS
Purity: ≥ 98%
CAS#: 1533426-72-0
Solubility: DMSO up to 50 mM
Chemical Name: 5,6-bis((E)-benzylideneamino)-2-mercaptopyrimidin-4-ol
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

SCR7 is a potent and selective inhibitor of non-homologous end joining (NHEJ). It inhibits joining of DSBs in cell-free DNA repair system, blocks Ligase IV-mediated joining by interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I, thereby leading to accumulation of DSBs within the cells, culminating into cytotoxicity. SCR7 inhibits NHEJ in a Ligase IV-dependent manner within cells, and activates the intrinsic apoptotic pathway. More importantly, SCR7 impedes tumor progression in mouse models, and when co-administered with DSB-inducing therapeutic modalities it enhances their sensitivity significantly. In addition, SCR7 can promote the efficiency of HDR 4–5-fold for CRISPR editing in both human and mouse cell lines.

How to Use:

In vitro:  SCR7 was used at 20-150 µM final concentration in vitro and in cellular assays for anti-cancer. SCR7 was used at 1 µM final concentration in CRISPR editing.

In vivo:  SCR7 was intraperitoneally (IP) dosed to mice at 20 mg/kg once per day.

Reference:

  1. 1. Srivastava M, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. (2012) Cell. 151(7):1474-87.
  2. 2. Chu VT, et al. Increasing the efficiency of homology-directed repair for CRISPR-Cas9-induced precise gene editing in mammalian cells. (2015) Nat Biotechnol. In press.


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


Description

Details

Product Information
Molecular Weight: 334.39
Formula: C18H14N4OS
Purity: ≥ 98%
CAS#: 1533426-72-0
Solubility: DMSO up to 50 mM
Chemical Name: 5,6-bis((E)-benzylideneamino)-2-mercaptopyrimidin-4-ol
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

SCR7 is a potent and selective inhibitor of non-homologous end joining (NHEJ). It inhibits joining of DSBs in cell-free DNA repair system, blocks Ligase IV-mediated joining by interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I, thereby leading to accumulation of DSBs within the cells, culminating into cytotoxicity. SCR7 inhibits NHEJ in a Ligase IV-dependent manner within cells, and activates the intrinsic apoptotic pathway. More importantly, SCR7 impedes tumor progression in mouse models, and when co-administered with DSB-inducing therapeutic modalities it enhances their sensitivity significantly. In addition, SCR7 can promote the efficiency of HDR 4–5-fold for CRISPR editing in both human and mouse cell lines.

How to Use:

In vitro:  SCR7 was used at 20-150 µM final concentration in vitro and in cellular assays for anti-cancer. SCR7 was used at 1 µM final concentration in CRISPR editing.

In vivo:  SCR7 was intraperitoneally (IP) dosed to mice at 20 mg/kg once per day.

Reference:

  1. 1. Srivastava M, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. (2012) Cell. 151(7):1474-87.
  2. 2. Chu VT, et al. Increasing the efficiency of homology-directed repair for CRISPR-Cas9-induced precise gene editing in mammalian cells. (2015) Nat Biotechnol. In press.


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


Reviews

  1. review Review by info@xcessbio.com
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    Question: 

    I was wondering if you could let me know what vehicle you use to inject SCR7 into mice?

     Your website reads:

    In vivo:  SCR7 was intraperitoneally (IP) dosed to mice at 20 mg/kg once per day.

    But doesn't mention the vehicle

     Our reply: 

    In that SCR7 Cell 2012 publication, the author did not mention what the dosing vehicle they used, so we do not know either. We recommend you to contact the paper author to know the details, or you can try some standard formulation (we can suggest some if you need). Please contact info@xcessbio.com for in vivo study formulation guidance

    Customer concern: 

    I think that in the paper they might have used DMSO, but I've been reading about it and mice don't seem to tolerate it well. We use vegetable oil to dissolve tamoxifen, which is also hydrophobic, for IP injections in mice. Do you think that's something that might work for SCR7? 

    Customer Solution after consulting: 

    Compound can be dissolved in water/metylcellulose, the compound will keep in the fridge only for a few days. 

    Customer question: 

    Would it be possible for you to aliquot a big amount of SCR7 (100 mg for example) into small aliquots (of 5 mg for example)?

    Our reply: 

    It is better to keep SCR7 as solid and take out exact amount to dissolve it into the right dosing formulation. SCR7 is a loose powder, so it is easy for you to weigh ~1 mg. Please not that most of our compounds with loose powder format could be measured out ~1 mg out of 5 mg or larger amount, with the correct scale (accuracy beyond 0.1 mg scale).  Our suggest is that customers test the compound in their system before ordering a big amount. For the feedback we got, it seems SCR7 is a tricky probe to use. Some people used it very well in their system but some people had difficulties to get the desired results. we assume it depends on the assay system.

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