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MedKoo Cat#: 533629 | Name: HOIPIN-8

Description:

WARNING: This product is for research use only, not for human or veterinary use.

HOIPIN-8 is a novel potent and selective inhibitor of linear ubiquitin chain assembly complex (LUBAC). HOIPIN-​8 suppressed the linear ubiquitination activity by recombinant LUBAC at an IC50 value of 11 nM, corresponding to a 255-​fold increase over that of HOIPIN-​1. Furthermore, as compared with HOIPIN-​1, HOIPIN-​8 showed 10-​fold and 4-​fold enhanced inhibitory activities on LUBAC- and TNF-​α-​induced NF-​κB activation respectively, without cytotoxicity. These results indicated that HOIPIN-​8 is a powerful tool to explore the physiological functions of LUBAC.

Chemical Structure

HOIPIN-8
HOIPIN-8
CAS#2519537-69-8 (free acid)

Theoretical Analysis

MedKoo Cat#: 533629

Name: HOIPIN-8

CAS#: 2519537-69-8 (free acid)

Chemical Formula: C23H16F2N4O3

Exact Mass: 434.1190

Molecular Weight: 434.40

Elemental Analysis: C, 63.59; H, 3.71; F, 8.75; N, 12.90; O, 11.05

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
2519537-69-8 (free acid) 2519537-70-1 (sodium)
Synonym
HOIPIN-8; HOIPIN 8; HOIPIN8
IUPAC/Chemical Name
(E)-2-(3-(2,6-difluoro-4-(1H-pyrazol-4-yl)phenyl)-3-oxoprop-1-en-1-yl)-4-(1-methyl-1H-pyrazol-4-yl)benzoic acid
InChi Key
UMAKCENGRSEXNB-HWKANZROSA-N
InChi Code
InChI=1S/C23H16F2N4O3/c1-29-12-17(11-28-29)13-2-4-18(23(31)32)14(6-13)3-5-21(30)22-19(24)7-15(8-20(22)25)16-9-26-27-10-16/h2-12H,1H3,(H,26,27)(H,31,32)/b5-3+
SMILES Code
O=C(C1=CC=C(C=C1/C=C/C(C2=C(C=C(C=C2F)C3=CNN=C3)F)=O)C4=CN(N=C4)C)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Nuclear factor-​κB (NF-​κB) is a crucial transcription factor family involved in the regulation of immune and inflammatory responses and cell survival. The linear ubiquitin chain assembly complex (LUBAC)​, composed of the HOIL-​1L, HOIP, and SHARPIN subunits, specifically generates Met1-​linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-​κB pathway

Preparing Stock Solutions

The following data is based on the product molecular weight 434.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Katsuya K, Oikawa D, Iio K, et al. Small-molecule inhibitors of linear ubiquitin chain assembly complex (LUBAC), HOIPINs, suppress NF-κB signaling. Biochem Biophys Res Commun. 2019;509(3):700‐706. doi:10.1016/j.bbrc.2018.12.164