2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC-IN-84

HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity.

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

HDAC-IN-84 Chemical Structure

HDAC-IN-84 Chemical Structure

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.

HDAC-IN-84 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

HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity[1].

IC50 & Target

HDAC1

0.0045 μM (IC50)

HDAC2

0.015 μM (IC50)

HDAC-3

0.013 μM (IC50)

HDAC4

>100 μM (IC50)

HDAC6

0.038 μM (IC50)

HDAC8

5.8 μM (IC50)

HDAC11

26 μM (IC50)

In Vitro

HDAC-IN-84 (95min) inhibits HDAC1, HDAC2, HDAC3, HDAC4, HDAC6, HDAC8 and HDAC11 with IC50 values of 0.0045, 0.015, 0.013, >100, 0.038, 5.8 and 26 μM, respectively[1].
HDAC-IN-84 (0.005-25 μM, 72 h) inhibits HL60, HPBALL, and K562 cells with IC50s of 76.8, 110.6 and 180.8 nM respectively[1].
HDAC-IN-84 (0.25 μM, 48 h) results in notable α-tubulin acetylation and higher PARP cleavage of HDAC6[1].
HDAC-IN-84 (0.25 μM, 48 h) induces Apoptosis in HL60 cells[1].
HDAC-IN-84 (0.15-0.2 μM, 24 h) induces cell cycle arrest in HL60 cells[1].
HDAC-IN-84 (2.5, 50 nM, 1 μM, 24 h) demonstrates excellent stability over the 24 h period monitored in human plasma at 37 °C[1].
HDAC-IN-84 (2.5, 50 nM, 1 μM, 48 h) binds with plasma protein with a mean of 99.0% over the observed concentration range with no concentration-dependency[1].
HDAC-IN-84 (0-1 μM) inhibits MV4-11 cells with an IC50 of 0.036 μM, exhibiting over a 7-fold increase inpotency compared to Vorinostat (HY-10221) [1].
HDAC-IN-84 (0-10 μM, 72 h) and Vorinosta (HY-10221) affects C1498 cell growth in a concentration-dependent manner with IC50s of 0.425 and 1.06 μM, respectively[1].
Comparison of In Vitro Pharmacokinetic Data of HDAC-IN-84 to Vorinostatas

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

HDAC-IN-84 Related Antibodies

Apoptosis Analysis[1]

vorinostatas HDAC-IN-84
log D 1.46 1.47
plasma stability/t1/2 75 min >24 h
KB/P 2.0 1.26
plasma protein binding 71% 99%
microsomal stability/t1/2( clearance category) 60 min 35.9 min
Cell Line: HL60 cells
Concentration: 0.25 μM
Incubation Time: 48 h
Result: Induced Apoptosis, leading to cytotoxic impacts on leukemia cells.

Cell Viability Assay[1]

Cell Line: K562, HL60, HPBALL cells
Concentration: 0.005-25 μM
Incubation Time: 72 h
Result: Inhibited HL60, HPBALL, and K562 cells with IC50s of 76.8, 110.6 and 180.8 nM respectively.

Western Blot Analysis[1]

Cell Line: HL60 cells
Concentration: 0.25μM
Incubation Time: 48 h
Result: Resulted in notable α-tubulin acetylation (indicating effective inhibition) of HDAC6.
Resulted in higher PARP cleavage (indicator of apoptosis induction).

Cell Cycle Analysis[1]

Cell Line: HL60 cells
Concentration: 0.15, 0.2 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest in leukemia cells.
In Vivo

HDAC-IN-84 (10 mg/kg, i.p., daily, 14 days) suppresses MV4-11 and C1498 cells growth in a preclinical leukemic xenograft mouse (NSG) model[1].
HDAC-IN-84 (10 mg/kg, i.p.) is characterized by a short elimination half-life of 0.35 h in three C57BL/6 mice. [1].
HDAC-IN-84 (20 mg/kg, i.p., daily, 21 days) exhibits significantly lower leukemia burden, with no significant differences in body weight in allograft leukemia model[1].
Pharmacokinetic Parameters (AUClast, Cmax, Tmax, and t1/2) Were Calculated According to a Noncompartmental Analysis (NCA) from the Blood Concentration of HDAC-IN-84 Based on Actual Blood Sampling Time Pre-Dose and Post-Dose

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

variable mouse 1 mouse 2 mouse 3 mean [±SD] vorinostat vorinostat
intraperitoneal 10 mg/kg per oral 50 mg/kg
Cmax (ng/mL) 1490 1030 1230 1250[±232] 501 580
Tmax (h) 0.25 0.25 0.25 0.25[±0] na 0.08
AUClast (h・ng/mL) 523 396 480 466[±65] 619 347
t1/2 0.275 0.554 0.227 0.352[±0.177] 0.75 0.8
Animal Model: preclinical leukemic xenograft mouse (NSG) model. Each mouse received 0.5 × 106 MV4-11 luc-GFP+ leukemic cells. After confirmation of tumor engraftment via monitoring bioluminescence-based in vivo imaging system (IVIS)[1] .
Dosage: 10 mg/kg
Administration: i.p., daily, 42 days
Result: Significantly suppressed the in vivo growth of MV4-11 leukemia cells as compared to the vehicle control.
Exhibited a minor (not significant) reduction in body weight.
Animal Model: Allograft leukemia model. In this model, leukemia is established by injecting (C57BL/6) derived murine AM L(C1498) cells by intravenous injection in immunocompetent wildtpye (C57BL/6) mice[1] .
Dosage: 20 mg/kg
Administration: i.p., daily, 21 days
Result: Exhibited significantly lower leukemia burden after the second treatment cycle, with this difference becoming more pronounced by day 19.
No significant differences in body weight were observed during the treatment course.
Molecular Weight

379.43

Formula

C17H21N3O5S
SMILES

O=C(C1=NC(C2=CC=C(OC)C=C2)=CS1)NOCCCCCC(NO)=O
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.

HDAC-IN-84 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:

HDAC-IN-84HDACApoptosisHistone deacetylasesDNA methylationleukemiaHDAC1HDAC2HDAC3HDAC4HDAC6HDAC8HDAC11Inhibitorinhibitorinhibit

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:
HDAC-IN-84
Cat. No.:
HY-170379
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

SAFETY DATA SHEET (SDS)

English - EN (0 KB) Français - FR (0 KB) Deutsch - DE (0 KB) Norwegian - NO (0 KB) Español - ES (0 KB) Swedish - SV (0 KB)

Request for HNMR Report

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