Home / Pharmacology / Enzymes / Ligases / Ubiquitin E3 Ligases / Ubiquitin E3 Ligase Inhibitors / KH-4-43

KH-4-43

Cat. No. 8091 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Selective CUL4 inhibitor
Chemical Name: 3-[1-(4-Chlorophenyl)-1H-pyrazol-4-yl]-7,8-dihydroxy-2-(trifluoromethyl)-4H-1-benzopyran-4-one
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for KH-4-43

KH-4-43 is a selective CUL4 inhibitor (Kd = 83 nM). KH-4-43 inhibits the ubiquitination of CK1α by CRL4CRBN in vitro. Treatment of cells with KH-4-43 causes accumulation of the E3 CRL4 substrate CDT1. KH-4-43 suppresses the growth of human tumor xenografts in mice.

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Technical Data for KH-4-43

M. Wt 422.74
Formula C19H10ClF3N2O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2813310-07-3
PubChem ID 164603779
InChI Key KDPAGFLLKCODNF-UHFFFAOYSA-N
Smiles O=C1C2=CC=C(C(O)=C2OC(C(F)(F)F)=C1C3=CN(C4=CC=C(C=C4)Cl)N=C3)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KH-4-43

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 8.45 20 with gentle warming
DMSO 21.14 50

Preparing Stock Solutions for KH-4-43

The following data is based on the product molecular weight 422.74. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.73 mL 23.66 mL 47.31 mL
2.5 mM 0.95 mL 4.73 mL 9.46 mL
5 mM 0.47 mL 2.37 mL 4.73 mL
25 mM 0.09 mL 0.47 mL 0.95 mL

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References for KH-4-43

References are publications that support the biological activity of the product.

Wu et al (2021) Inhibitors of cullin-RING E3 ubiquitin ligase 4 with antitumor potential. Proc.Natl.Acad.Sci.U.S.A. 118 e2007328118 PMID: 33602808

If you know of a relevant reference for KH-4-43, please let us know.

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Keywords: KH-4-43, KH-4-43 supplier, KH443, inhibitors, inhibits, antitumor, antitumour, mouse, Ubiquitin, E3, Ligases, 8091, Tocris Bioscience

Citations for KH-4-43

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

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