RK-0080552
RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma.
For research use only. We do not sell to patients.
- CAS No.: 313527-11-6
- Formula: C12H6N6O2
- Molecular Weight:266.22
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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All Histone Methyltransferase Isoforms
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Biological Activity
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NSD2 |
RK-0080552 (0-5 μM; 72 h) exerts significant, dose-dependent cytotoxicity in t (4;14)+ human multiple myeloma cell lines (KMS28-BM, KMS34, KMS26, NCI-H929, KMS11)[1].
RK-0080552 (0-5 μM; 1-3 days) reduces H3K36me2 levels and increases H3K27me3 levels in t (4;14)+ human multiple myeloma cell lines (KMS28-BM, KMS34, KMS26) in a dose- and time-dependent manner[1].
RK-0080552 (0-5 μM; 1-2 days) downregulates the expression of IRF4, a key growth and survival gene in multiple myeloma (MM)[1].
RK-0080552 (5 μM; 24 h) specifically induces apoptosis in primary t (4;14)+ human multiple myeloma CD138+ cells, with no effect on normal CD3+ T lymphocytes[1].
RK-0080552 (5 μM; 24 h) reduces global H3K36me2 levels and specifically decreases H3K36me2 enrichment at the IRF4 gene, particularly in intronic regions, in t (4;14)+ human multiple myeloma KMS34 cells[1].
RK-0080552 (0.5-4 μM; 24-72 h) exerts a synergistic cytotoxic effect with Pomalidomide (HY-10984) in t (4;14)+ human multiple myeloma cell lines (KMS28-BM, KMS34, KMS26, NCI-H929), and this effect correlates with enhanced downregulation of IRF4 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:t(4;14)+ human multiple myeloma (MM) cell lines (KMS28-BM, KMS34, KMS26, NCI-H929, KMS11), t(4;14)- human MM cell lines (RPMI8226, KMM.1, SKMM1, JJN3, KMS21)
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Concentration:0, 1, 2, 3, 4, 5 μM
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Incubation Time:72 h
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Result:Induced significant dose-dependent cytotoxicity in all tested t(4;14)+ MM cell lines.
Confirmed induction of cell death rather than cell cycle arrest in t(4;14)+ MM cell lines via flow cytometric analysis.
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Cell Line:t(4;14)+ human MM cell lines (KMS28-BM, KMS34, KMS26)
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Concentration:0, 3, 4, 5 μM
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Incubation Time:24 h, 48 h
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Result:Reduced IRF4 protein levels in a dose- and time-dependent manner in all tested t(4;14)+ MM cell lines.
| Species | Dose | Route | AUC | Cmax | T1/2 | Plasma Concentration |
|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 13.1 μM·h | 8.3 μM | 0.84 h | 7.12 μM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (male)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; 5 times a week; 3 weeks
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Result:Suppressed subcutaneous KMS34 tumor growth.
Reduced tumor cell numbers, induced apoptosis, decreased H3K36me2 levels, and suppressed IRF4 expression in human CD138-expressing tumor cells.
Slightly prolonged overall survival of mice bearing intravenous KMS26 tumors.
Chemical Information
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CAS No. 313527-11-6
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Molecular Weight 266.22
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Formula C12H6N6O2
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SMILES
NC1=NON=C1C(N=N2)=NC3=C2C(C4=C3C=CC=C4)=O
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Synonyms
RK-552
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RK-0080552 Related Classifications
HY-172614 Related Classifications
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