2. Cell Cycle/DNA Damage Epigenetics Apoptosis Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. HDAC Apoptosis Bcr-Abl HSP
  4. MRLB-223

MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma.

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MRLB-223

MRLB-223 Chemical Structure

CAS No. : 937727-03-2

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MRLB-223 Related Antibodies

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Description

MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma[1].

IC50 & Target

HDAC1

 

HDAC2

 

HSP90

 

In Vitro

MRLB-223 (0.2-10 μM; 24-48 h) induces concentration-dependent apoptosis in Eμ-myc lymphoma cells via the intrinsic apoptotic pathway with delayed kinetics, with an IC70 of 5 μM at 24 hours and 0.5 μM at 48 hours[1].
MRLB-223 (0-12 μM; 24 h) induces concentration-dependent apoptosis in Eμ-myc and Eμ-myc/p53-/- lymphoma cells independently of p53, while overexpression of Bcl-2 blocks this apoptotic effect[1].
MRLB-223 (0-30 μM; 24-72 h) induces concentration-dependent cell death in FDCP-1 mouse myeloid cells with delayed kinetics, requiring longer incubation times for maximal effect[1].
MRLB-223 (0-26 μM; 72 h) induces concentration-dependent cell death in FDCP-1/Bcr-Abl and FDCP-1/Bcr-AblT315I cells with delayed kinetics, and Bcr-Abl degradation occurs as a downstream consequence of caspase-mediated apoptosis[1].
MRLB-223 (10 μM; 24 h) induces hyperacetylation of Hsp90 in FDCP-1/Bcr-Abl cells despite lacking activity against HDAC6[1].
MRLB-223 (0-16 μM; 72 h) induces concentration-dependent cell death in FDCP-1/Bcr-Abl cells, and knockdown of HDAC6 does not enhance this apoptotic effect[1].

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

MRLB-223 Related Antibodies

Cell Viability Assay[1]

Cell Line: Eμ-myc, Eμ-myc/p53-/-, and Eμ-myc/Bcl-2 lymphoma cells
Concentration: 0-12 μM
Incubation Time: 24 h
Result: Induced concentration-dependent PI uptake in Eμ-myc and Eμ-myc/p53-/- cells, with both cell lines showing similar sensitivity.
Suppressed MRLB-223-mediated tumor cell death was observed when Bcl-2 was overexpressed.

Cell Viability Assay[1]

Cell Line: FDCP-1/Bcr-Abl and FDCP-1/Bcr-Abl(T315I) mouse myeloid cells
Concentration: 0-26 μM (72 h PI uptake assay); 5, 10 μM (48 h Bcr-Abl degradation assay)
Incubation Time: 72 h (PI uptake assay); 48 h (Bcr-Abl degradation assay)
Result: Induced concentration-dependent PI uptake in FDCP-1/Bcr-Abl and FDCP-1/Bcr-Abl(T315I) cells at 72 hours, with both cell lines showing equivalent sensitivity.
Induced Bcr-Abl degradation concomitant with apoptosis in cells treated with 5 or 10 μM for 48 hours.
Suppressed apoptosis and maintained Bcr-Abl expression when co-treated with the caspase inhibitor Q-VD-OPh for 48 hours.
In Vivo

MRLB-223 (15 mg/kg; i.p.) exerts antitumor activity in mice bearing Eμ-myc lymphoma, extending the median survival to 42 days, but its histone hyperacetylation and antitumor kinetics are delayed compared with broad-spectrum HDAC inhibitors[1].

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

Animal Model: C57BL/6 (6- to 8-week-old; injected intravenously with 5×105 Eμ-myc lymphoma cells)[1]
Dosage: 15 mg/kg (therapy studies; in vivo apoptosis assays; FDG-PET analysis)
Administration: i.p.; daily, continuous (therapy studies); single dose (in vivo apoptosis assays; FDG-PET analysis)
Result: Reduced average peripheral white blood cell counts to 23.9×103/μL by day 21 and 33.8×103/μL by day 35 (vehicle controls reached 39.2×103/μL by day 21).
Increased median mouse survival to 42 days (vehicle controls had 33 days).
Induced delayed histone H3 and H4 hyperacetylation in lymphoma cells, with minimal acetylation at 2 hours post-dose and gradual increases over time.
Showed no reduction in lymph node FDG uptake at 4 hours post-dose, but a decrease was observed by 48 hours post-dose.
Molecular Weight

449.53

Formula

C23H23N5O3S
CAS No.
SMILES

O=C1OC2(CCN(CC2)C3=NC=C(C(NC4=C(N)C=CC(C5=CC=CS5)=C4)=O)C=C3)CN1
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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MRLB-223 Related Classifications

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  • 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:

MRLB-223937727-03-2MRLB223MRLB 223HDACApoptosisBcr-AblHSPHistone deacetylasesHeat shock proteinstumor cell apoptosisFDCP-1 mouse myeloid cellsp53histone hyperacetylationHsp90 hyperacetylationEμ-myc lymphomasHDAC1intrinsic apoptotic pathwayHDAC2Inhibitorinhibitorinhibit

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