2. NF-κB
  3. IKK
  4. HPN-01

HPN-01 

Cat. No.: HY-135366 Purity: 98.40%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 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  

* Please select Quantity before adding items.

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

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Based on 1 publication(s) in Google Scholar

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IKK-α IKK-β IKK IKKε TBK1

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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].

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

401.87

Appearance

Solid

Formula

C19H16ClN3O3S
CAS No.
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)

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
10 mM 0.2488 mL 1.2442 mL 2.4884 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.40%

COA (249 KB) LCMS (270 KB)

Handling Instructions (2659 KB)
References
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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.

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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)
× = ×
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Keywords:

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

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