2. Metabolic Enzyme/Protease Epigenetics
  3. Oxidative Phosphorylation Epigenetic Reader Domain
  4. FHD-286

FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia.

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

FHD-286 Chemical Structure

FHD-286 Chemical Structure

CAS No. : 2671128-05-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 450 In-stock
10 mg USD 700 In-stock
25 mg USD 950 In-stock
50 mg USD 1250 In-stock
100 mg USD 1650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

FHD-286 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE FHD-286

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia[1].

In Vitro

FHD-286 (10 to 100 nM) for 7 days induces differentiation followed by loss of viability of AML cell lines and PD AML cells with MLL rearrangement (r), mutant (mt) NPM1 and chromosome 3q26 lesions (with EVI1 overexpression). Treatment with FHD-286 causes whole-genome, concordant, up- or down-regulations in ATAC-Seq peaks and RNA-Seq-determined mRNA expressions of specific loci, associated with significant reduction in the gene-sets of targets of MYC, mTORC1, E2F, Interferon-gamma, IL6-JAK-STAT3, as well as of inflammatory response and oxidative phosphorylation genes. QPCR analyses determined significant reduction in mRNA expression of MYC, SPI1 and BCL2 genes. Mass spectrometry on AML cell lysates treated with FHD-286 showed log2 fold-reductions in c-Myc, SPI1, MEF2C, KMT2C and CDK4 (in MOLM13) and in EVI1, c-Myb, CDK6 and c-Myc (in AML191) cells[1].

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

FHD-286 Related Antibodies
In Vivo

FHD-286 (1.5 mg/kg; oral administration; for 10 days) increases in IFNγ and Th1-type chemokine CXCL10 levels[2].

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

Animal Model: B16F10 tumor-bearing mice[2]
Dosage: 1.5 mg/kg
Administration: Oral administration; for 10 days
Result: Increased in IFNγ and Th1-type chemokine CXCL10 levels.
Molecular Weight

562.66

Formula

C24H30N6O6S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC[C@@H](C(NC1=NC(C2=CC=CC(N3C[C@@H](O[C@@H](C3)C)C)=N2)=CS1)=O)NC(C4=CN(C=C4)S(C)(=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (444.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7773 mL 8.8864 mL 17.7727 mL
5 mM 0.3555 mL 1.7773 mL 3.5545 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.06%

COA (249 KB) HNMR (297 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7773 mL 8.8864 mL 17.7727 mL 44.4318 mL
5 mM 0.3555 mL 1.7773 mL 3.5545 mL 8.8864 mL
10 mM 0.1777 mL 0.8886 mL 1.7773 mL 4.4432 mL
15 mM 0.1185 mL 0.5924 mL 1.1848 mL 2.9621 mL
20 mM 0.0889 mL 0.4443 mL 0.8886 mL 2.2216 mL
25 mM 0.0711 mL 0.3555 mL 0.7109 mL 1.7773 mL
30 mM 0.0592 mL 0.2962 mL 0.5924 mL 1.4811 mL
40 mM 0.0444 mL 0.2222 mL 0.4443 mL 1.1108 mL
50 mM 0.0355 mL 0.1777 mL 0.3555 mL 0.8886 mL
60 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7405 mL
80 mM 0.0222 mL 0.1111 mL 0.2222 mL 0.5554 mL
100 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4443 mL
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FHD-286 Related Classifications

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:

FHD-2862671128-05-3FHD286FHD 286Oxidative PhosphorylationEpigenetic Reader DomainInhibitorinhibitorinhibit

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