2. NF-κB
  3. IKK
  4. HPN-01

HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.

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

HPN-01 Chemical Structure

HPN-01 Chemical Structure

CAS No. : 928655-63-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

HPN-01 Related Antibodies

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IKK-α IKK-β IKK IKKε TBK1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2[1].

IC50 & Target[1]

IKK-α

6.4 (pIC50)

IKK-β

7.0 (pIC50)

IKK-ε

<4.8 (pIC50)

In Vitro

HPN-01 effectively suppress LPS-stimulated secretion of TNF-α, IL-1β, and IL-6 from human PBMCs (pIC50=6.1, 6.4, and 5.7, respectively). HPN-01 also inhibits TNF-α-induced NF-κB nuclear translocation in human lung fibroblast cells (pIC50=5.7)[1].
HPN-01 inhibits the expression of SREBP-1and SREBP-2 in cultured primary human hepatocytes with IC50s of 1.71 μΜ and 3.43 μΜ, respectively. HPN-01 is being development for the treatment of nonalcoholic fatty liver disease (NAFLD)[2].

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

HPN-01 Related Antibodies
Molecular Weight

401.87

Formula

C19H16ClN3O3S
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(C1=C(N)C(C2=CC=C(S(=O)(N)=O)C=C2)=CC(C3=CC=C(Cl)C=C3)=C1)N
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 : 100 mg/mL (248.84 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 2.4884 mL 12.4418 mL 24.8837 mL
5 mM 0.4977 mL 2.4884 mL 4.9767 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
×
Volume
×
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

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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: 98.61%

SDS (251 KB)

COA (249 KB) LCMS (94 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 2.4884 mL 12.4418 mL 24.8837 mL 62.2092 mL
5 mM 0.4977 mL 2.4884 mL 4.9767 mL 12.4418 mL
10 mM 0.2488 mL 1.2442 mL 2.4884 mL 6.2209 mL
15 mM 0.1659 mL 0.8295 mL 1.6589 mL 4.1473 mL
20 mM 0.1244 mL 0.6221 mL 1.2442 mL 3.1105 mL
25 mM 0.0995 mL 0.4977 mL 0.9953 mL 2.4884 mL
30 mM 0.0829 mL 0.4147 mL 0.8295 mL 2.0736 mL
40 mM 0.0622 mL 0.3110 mL 0.6221 mL 1.5552 mL
50 mM 0.0498 mL 0.2488 mL 0.4977 mL 1.2442 mL
60 mM 0.0415 mL 0.2074 mL 0.4147 mL 1.0368 mL
80 mM 0.0311 mL 0.1555 mL 0.3110 mL 0.7776 mL
100 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6221 mL
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HPN-01 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:

HPN-01928655-63-4HPN01HPN 01IKKIκB kinaseI kappa B kinaseLPSsecretionPBMCNF-κBnucleartranslocationNAFLDInhibitorinhibitorinhibit

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