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

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.

For research use only. We do not sell to patients.

PTG-0861 Chemical Structure

PTG-0861 Chemical Structure

CAS No. : 2494082-34-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PTG-0861 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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].

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

PTG-0861 Related Antibodies

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
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].

MedChemExpress (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
Molecular Weight

360.24

Formula

C15H9F5N2O3
CAS No.
SMILES

O=C(NCC1=CC=C(C(NO)=O)C=C1)C2=C(F)C(F)=C(F)C(F)=C2F
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PTG-0861 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PTG-0861
Cat. No.:
HY-150586
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.