2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. PTG-0861

PTG-0861 是一种选择性的组蛋白去乙酰酶 (HDAC6) 抑制剂，其 IC50 值为 5.92 nM。PTG-0861 可诱导细胞凋亡 (apoptosis)，用于急性髓性白血病、多发性骨髓瘤等血液癌症相关疾病的研究。

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PTG-0861 Chemical Structure

PTG-0861 Chemical Structure

CAS No. : 2494082-34-5

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PTG-0861 相关抗体

Top Publications Citing Use of Products

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers[1].

IC50 & Target[1]

HDAC6

5.92 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Fibroblast IC50
11.5 μM
Compound: 54; PTG-0861
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
Fibroblast IC50
14.6 μM
Compound: 54; PTG-0861
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
HUVEC IC50
10.3 μM
Compound: 54; PTG-0861
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MM1.S IC50
1.9 μM
Compound: 54; PTG-0861
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MV4-11 IC50
1.85 μM
Compound: 1
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.85 μM
Compound: 54; PTG-0861
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
RPMI-8226 IC50
4.94 μM
Compound: 54; PTG-0861
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
体外研究
(In Vitro)

PTG-0861 (compound 54) (0.1-5 μM, 6 hours) stimulates the expression of acetylated a-tubulin and has inhibitory activity against HDAC6 with the IC50 value of 0.59 μM[1].
PTG-0861 (compound 54) (0-4 μM, 18 hours) can induce apoptosis in a dose-dependent manner and has some cytotoxic effect[1].

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

PTG-0861 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1-5 μM
Incubation Time: 6 hours
Result: Induced the accumulation of acetylated a-tubulin expression at 500 nM.

Immunofluorescence[1]

Cell Line: HeLa cells
Concentration: 0-2 μM
Incubation Time: 6 hours
Result: Increased levels of acetylated a-tubulin at 0.1 μM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0-4 μM
Incubation Time: 18 hours
Result: Induced about 18% cells late apoptosis at 4 μM while at low dose 0.25 μM only about 5%.

Cell Cytotoxicity Assay[1]

Cell Line: Hematological cancer cell lines MV4-11, MM.1S, and RPMI 8226
Concentration: 1.24-4.94 μM
Incubation Time: 72 hours
Result: Showed cytotoxic effects on MV4-11, MM.1S, and RPMI 8226 with the IC50 value of 1.85 μM，1.9 μM，4.94 μM, respectively.

Cell Line:
Concentration:
Incubation Time:
Result: Result: The pharmacokinetic parameters of PTG-0861 in vitro
Parameter PTG-0861
Percent Remaining (%) 0 min 100.00
Percent Remaining (%) 30 min 96.41
Percent Remaining (%) 60 min 97.98
Percent Remaining (%) 120 min 97.08
T1/2 (min) ∞
T1/2 (min) 50.85 ± 3.37
CLint (mL/min/106 cells) 27.32 ± 1.81
-Log Pe 5.66 ± 0.02
Papp (A-B) (10 6, cm/s) 1.33 ± 0.03
Papp (B-A) (10 6, cm/s) 0.94 ± 0.13
Efflux Ratio 0.71 ± 0.08
体内研究
(In Vivo)

PTG-0861 (compound 54) (oral administration, 20 mg/kg, everyday, 5 days) has no effect on weight and no obvious toxicity in CD1 mice[1].

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

Animal Model: CD1 mice[1]
Dosage: 20 mg/kg
Administration: Oral administration; everyday; 5 days
Result: No weight loss in mice and no obvious toxicity.
Animal Model: Male CD1 mice[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; once
Result: The pharmacokinetic parameters of PTG-0861 in vivo
Parameter PTG-0861
half-life 0.25 h
Cmax 526 ng/mL
AUClast 190 h∗ng/mL
AUCinf 219 h∗ng/mL
AUC Extr(%) 0.324
MRT(h) 0.350
AUC/D(h∗mg/mL) 9.5
分子量

360.24

Formula

C15H9F5N2O3
CAS 号
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

PTG-0861 相关分类

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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:

PTG-08612494082-34-5PTG0861PTG 0861HDACApoptosisHistone deacetylaseshistone deacetylase 6 (HDAC6)acute myeloid leukaemiamultiple myelomahematological cancersInhibitorinhibitorinhibit

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