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 是一种高效的 PIM/HDAC 抑制剂，其 IC50 值为 0.11 μM，通过抑制 PIM1 激酶 (IC50  为 2.6 nM) 和选择性抑制 HDAC6 (IC50 为 8 nM) 的双重机制发挥协同抗增殖作用。PIM-1/HDAC-IN-2 能显著诱导 PARP 裂解，从而促使细胞周期停滞在 G1 期，S 期细胞减少。PIM-1/HDAC-IN-2 在 MV4-11 肿瘤移植模型中显示出显著的抗癌效果，且无明显毒性[1]。

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PIM-1/HDAC-IN-2 Chemical Structure

PIM-1/HDAC-IN-2 Chemical Structure

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Customer Review

PIM-1/HDAC-IN-2 相关抗体

Top Publications Citing Use of Products

查看 Pim 亚型特异性产品:

查看所有亚型
PIM1 PIM2 PIM3

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 (IC50 = 2.6 nM) and selectively inhibiting HDAC6 (IC50  = 8 nM). 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)

体外研究
(In Vitro)

PIM-1/HDAC-IN-2 (96 h) 展现出对多种肿瘤细胞的毒性，其 IC50 值分别为：0.11 μM (MV4-11)，3.56 μM (MOLM-13)，1.71 μM (RPMI 8226)，7.09 μM (MM.1S)[1]。

与单一靶向 HDACi (SAHA) (HY-10221) (IC50 值 为 0.53 μM) 或 PIM 激酶抑制剂 C28 (HY-153896) (IC50值为 0.98 μM) 相比，PIM-1/HDAC-IN-2 (96 h) 在 MV4-11 细胞中表现出了最佳抑制效果，IC50 值为 0.11 μM)[1]。

PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) 显著增强 MV4-11 细胞中的 PARP 裂解，且具有浓度依赖性[1]。

PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) 在 MV4-11 细胞中显示出显著的诱导细胞凋亡能力[1]。

PIM-1/HDAC-IN-2 (0.1-1 μM, 48 h) 诱导 MV4-11 细胞周期在 G1 期发生浓度依赖性阻滞，同时 S 期细胞数量减少[1]。

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

PIM-1/HDAC-IN-2 相关抗体:

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.
体内研究
(In Vivo)

PIM-1/HDAC-IN-2 (50 mg/kg，25 mg/kg，腹腔注射，连续21天) 在 MV4-11 肿瘤移植模型中显示出良好的抗肿瘤效果和耐受性[1]。

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.
分子量

607.70

Formula

C34H37N7O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PIM-1/HDAC-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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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