2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. 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.

RK-0080552

RK-0080552 Chemical Structure

CAS No. : 313527-11-6

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RK-0080552 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1].

In Vitro

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.

RK-0080552 Related Antibodies

Cell Cytotoxicity Assay[1]

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)
Concentration: 0, 1, 2, 3, 4, 5 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: t(4;14)+ human MM cell lines (KMS28-BM, KMS34, KMS26)
Concentration: 0, 3, 4, 5 μM
Incubation Time: 24 h, 48 h
Result: Reduced IRF4 protein levels in a dose- and time-dependent manner in all tested t(4;14)+ MM cell lines.
Parmacokinetics
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
In Vivo

RK-552 (i.p.; 5-20 mg/kg; 5 times per week for 3 consecutive weeks) significantly inhibits subcutaneous tumor growth of t (4;14)+ multiple myeloma in NOD/SCID mice by reducing H3K36me2 levels and downregulating IRF4[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID (male)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; 5 times a week; 3 weeks
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.
Molecular Weight

266.22

Formula

C12H6N6O2
CAS No.
SMILES

NC1=NON=C1C(N=N2)=NC3=C2C(C4=C3C=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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RK-0080552 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-0080552313527-11-6RK-552RK0080552RK 0080552RK552RK 552Histone MethyltransferaseApoptosisSET7/9NSD2IRF4multiple myeloma with t(4;14)t(4;14)+ human MM cell linesNOD/SCID miceMYCSLAMF7G9ahistone H3 lysine 36 dimethylationInhibitorinhibitorinhibit

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