PIM-1/HDAC-IN-2
PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
For research use only. We do not sell to patients.
- CAS No.: 3103925-33-0
- Formula: C34H37N7O4
- Molecular Weight:607.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PIM1 2.6 nM (IC50) |
HDAC6 8 nM (IC50) |
HDAC1 41 nM (IC50) |
HDAC10 72 nM (IC50) |
HDAC3 101 nM (IC50) |
HDAC11 105 nM (IC50) |
HDAC8 225 nM (IC50) |
HDAC2 341 nM (IC50) |
HDAC5 379 nM (IC50) |
HDAC7 690 nM (IC50) |
HDAC9 1084 nM (IC50) |
HDAC4 3456 nM (IC50) |
PIM-1/HDAC-IN-2 (Compound 22) (96 h) shows cytotoxicity in tumor cells with IC50 of 0.11 μM (MV4-11), 3.56 μM (MOLM-13), 1.71 μM (RPMI 8226), 7.09 μM (MM.1S), respectively[1].
PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) significantly enhances the PARP cleavage in MV4-11 cells in a concentration-dependent manner[1].
PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) demonstrates a significantly apoptosis-inducing capability in MV4-11 cells[1].
PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) induces the concentration-dependent arrest of the cell cycle in G1 phase, accompanied by a reduction in the number of cells in S phase in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, 1 μM
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Incubation Time:48 h
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Result:Demonstrated a significantly superior apoptosis-inducing capability (92.4%) compared to C28 (20.2%), a slightly enhanced effect relative to SAHA (89.2%), and was comparable to C28 + SAHA (0.5 + 0.5 μM) (94.8%) at 1 μM.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, 1 μM
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Incubation Time:48 h
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Result:Induced the concentration-dependent arrest of the cell cycle in G1 phase.
Reduced the number of cells in S phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 xenograft model established in female BALB/c-Nude mice (6-8 weeks) [1].
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Dosage:50 mg/kg, 25 mg/kg
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Administration:Daily intraperitoneal injection (i.p.), at the corresponding doses for 21 days.
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Result:Showed TGI values of 81.3% (50 mg/kg) and 45.9% (25 mg/kg).
Exhibited superior in vivo antitumor activity over the positive control C28 and SAHA at the same dose.
Had no significant weight loss or toxic effects.
Induced necrosis of MV4-11 tumor tissues but showed no apparent toxicity of heart, liver, spleen, lungs, and kidneys (H&E staining).
Resulted in the significant PARP cleavage, compared to the positive control C28 and SAHA at the same dose.
Chemical Information
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CAS No. 3103925-33-0
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Molecular Weight 607.70
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Formula C34H37N7O4
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SMILES
O=C1N(C(NC2CCN(CC2)CC3=CC=C(C=C3)/C=C/C(NO)=O)=NC4=C1C=CC=C4C5=CC6=C(N5)[C@H](NC6=O)C)C7(C)CC7
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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)
PIM-1/HDAC-IN-2 Related Classifications
HY-174302 Related Classifications
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