2. JAK/STAT Signaling Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Pim HDAC PARP Apoptosis
  4. PIM-1/HDAC-IN-2

PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. 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.

PIM-1/HDAC-IN-2 Chemical Structure

PIM-1/HDAC-IN-2 Chemical Structure

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PIM-1/HDAC-IN-2 Related Antibodies

Top Publications Citing Use of Products

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PIM1 PIM2 PIM3

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. 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].

IC50 & Target[1]

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)

In Vitro

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 (96 h) shows potent antiproliferative activity in MV4-11 cells (IC50 = 0.11 μM) compared to single-targeted HDACi (SAHA) (HY-10221) (IC50 = 0.53 μM) or PIM kinase inhibitor C28 (IC50 = 0.98 μM)[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.

PIM-1/HDAC-IN-2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 48h
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.
In Vivo

PIM-1/HDAC-IN-2 (Compound 22) (50 mg/kg, 25 mg/kg, i.p., daily for 21 days) shows antitumor efficacy and well tolerance in MV4-11 xenograft models[1].

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

Animal Model: MV4-11 xenograft model established in female BALB/c-Nude mice (6−8 weeks) [1].
Dosage: 50 mg/kg, 25 mg/kg
Administration: Daily intraperitoneal injection (i.p.), at the corresponding doses for 21 days.
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.
Molecular Weight

607.70

Formula

C34H37N7O4
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PIM-1/HDAC-IN-2 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:

PIM-1/HDAC-IN-2PimHDACPARPApoptosisPim kinasesHistone deacetylasespoly ADP ribose polymerase PIM-1HDAC6PIM-1/HDAC inhibitorsMV4-11 cellMV4-11 xenograft modelAnticancerInhibitorinhibitorinhibit

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