2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. RK-582

RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model.

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RK-582 Chemical Structure

RK-582 Chemical Structure

CAS No. : 2171388-28-4

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Description

RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model[1].

IC50 & Target

IC50: 36.1 nM (TNKS1/PARP5A), 18.168 nM (PARP1)[1]
Molecular Weight

510.60

Formula

C27H35FN6O3
CAS No.
SMILES

O=C(N1C)C2(CCN(C(NC3=C4CCCN3C)=NC4=O)CC2)C(C1=CC(N(C[C@@H]5C)C[C@H](O5)C)=C6)=C6F
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RK-582 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RK-5822171388-28-4RK582RK 582PARPpoly ADP ribose polymeraseoral effectivexenograft modelCOLO-320DMInhibitorinhibitorinhibit

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