2. Apoptosis
  3. Apoptosis
  4. MM927

MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC).

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MM927

MM927 Chemical Structure

CAS No. : 3065567-21-4

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MM927 Related Antibodies

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Description

MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC)[1].

In Vitro

MM927 (72 h) inhibits viability of HCT116 cells (IC50 = 53 nM) and MOLM-13 cells (IC50 = 92 nM)[1].
MM927 (0.5 μM, 24 h) induces half-mer polysomes and reduces free 60S/80S peaks in polysome profiles of HCT116 NVL WT cells[1].
MM927 (3 μM, 6 h) shifts newly synthesized eL36-SNAP (60S subunit marker) to non-ribosomal fractions and depletes it from 60S/80S/polysome fractions in HCT116 cells[1].
MM927 (3 μM, 24 h) causes reduction in cytoplasmic signal of newly synthesized eL36-SNAP (60S) and retains it in nucleolar foci (colocalized with Fibrillarin) in HCT116 NVL WT cells[1].
MM927 (0.5 μM, 24-48 h) induces G1/S and G2/M cell cycle arrest in HCT116 mock cells[1].
MM927 (3 μM, 2-3 days) triggers apoptosis in MOLM-13 cells, as shown by decreased procaspase-3 and increased cleaved caspase-3 levels, and high Annexin V-positive cell rates[1].
MM927 (0.051 μM, 72 h) inhibits the viability of HCT116 NVLAID/AID cells expressing ectopic human NVL with an IC50 of 0.051 μM, and inhibits HCT116 NVLAID/AID cells expressing ectopic mouse NVL with an IC50 of 0.207 μM[1].

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

MM927 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 3 μM
Incubation Time: 2, 3 days
Result: Induced apoptosis in MOLM-13 cells.
Decreased procaspase-3.
Increased cleaved caspase-3 levels, and high Annexin V-positive cell rates.
In Vivo

MM927 (35 mg/kg, i.p., twice daily, 21 days) reduces the growth of HCT116 NVL WT tumor xenografts and decreases tumor burden in NSG mice, with no effect on HCT116 NVL R403WCRISPR tumor xenografts[1].
MM927 (35 mg/kg, i.p., twice daily, 14 days) causes reduction in leukemic disease burden in NSG mice[1].
MM927 (35 mg/kg, i.p., twice daily, 3 days) increases nuclear p53 staining and reduces Ki-67-positive cell staining in HCT116 NVL WT tumor xenografts of NSG mice[1].

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

Animal Model: HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 21 days
Result: Achieved tumor growth inhibition (TGI) in HCT116 NVL WT tumor xenografts of NSG mice.
Reduced tumor burden at the end of treatment.
Showed no effect on HCT116 NVL R403WCRISPR tumor xenografts.
Showed no significant changes in body weight, no significant alterations in hemoglobin, platelets, liver Enzymes (ALT, AST).
Animal Model: Luciferase-expressing MOLM-13 cells (1 × 106) were intravenously injected into the tail vein of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 14 days
Result: Achieved a 7-fold reduction in leukemic disease burden.
Caused a 9-fold decrease in MOLM-13 cell percentage in bone marrow and a 15-fold decrease in peripheral blood.
Animal Model: HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 3 days
Result: Reduced Ki-67-positive (proliferating) cell staining in HCT116 NVL WT tumor xenografts of NSG mice, with few cells showing co-localization of p53 and Ki-67.
Molecular Weight

487.50

Formula

C26H18FN3O4S
CAS No.
SMILES

O=C1OC2=CC=C(C(NC3=CC=C4C(SC5=CC(F)=CC=C5C(N4CC#CC)=O)=C3)=O)C=C2N1C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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MM927 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:

MM9273065567-21-4MM 927MM-927Apoptosisacute myeloid leukemiacolorectal cancerNVLHCT116 cellsInhibitorinhibitorinhibit

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