| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
TEAD[1]
IK-930 targets TEAD (Transcriptional Enhancer Associate Domain) transcription factors, which are the downstream effectors of the Hippo signaling pathway. TEAD proteins interact with YAP/TAZ coactivators to drive transcription of genes involved in cell proliferation, survival, and oncogenesis. IK-930 inhibits TEAD activity by directly blocking autopalmitoylation, a post-translational modification required for TEAD function. This prevents TEAD from interacting with YAP/TAZ and activating target gene expression. |
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| ln Vitro |
IK-930 demonstrates potent TEAD inhibitory activity with an EC50 of less than 0.1 μM. It is inactive in a broad panel of kinases, receptors, and transporters, indicating high selectivity for TEAD. The compound's selectivity profile minimizes off-target effects, making it a valuable tool for studying TEAD-dependent biology. In vitro studies have characterized its effects on TEAD-mediated transcription and cell proliferation in various cancer cell lines.
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| ln Vivo |
IK-930 (compound I-32) (10 mg/kg; po) in BALB/c mice shows favorable pharmacokinetic characteristics, with an AUC 0-last of 4581 ng*h /mL and a Cmax of 1088 ng/mL[1].
IK-930 (10 mg/kg; p.o.) demonstrates good pharmacokinetic properties in BALB/c mice, with a Cmax of 1088 ng/mL and an AUC0-last of 4581 ng·h/mL. These parameters indicate favorable oral bioavailability and systemic exposure. The compound's oral activity and favorable PK profile make it a promising candidate for further in vivo efficacy studies in cancer models. IK-930's efficacy in tumor models is an area of ongoing research. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for IK-930 typically involves a TEAD autopalmitoylation assay. Recombinant TEAD protein is incubated with palmitoyl-CoA and varying concentrations of IK-930. The incorporation of palmitate into TEAD is measured using radiolabeled palmitoyl-CoA or a fluorescence-based detection method. Alternatively, a YAP/TAZ-TEAD protein-protein interaction assay can be performed using surface plasmon resonance or ELISA to measure the compound's ability to disrupt the interaction between YAP/TAZ and TEAD.
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| Cell Assay |
The in vitro cellular assay for IK-930 typically uses cancer cell lines with active YAP/TAZ-TEAD signaling. Cells are treated with varying concentrations of IK-930, and TEAD-dependent transcriptional activity is measured using a TEAD-responsive luciferase reporter assay. Cell proliferation and viability are assessed using standard assays such as CellTiter-Glo or MTT. The compound's effects on TEAD target gene expression can be evaluated by qPCR or Western blot. Its selectivity is confirmed by screening against a panel of kinases and receptors.
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| Animal Protocol |
In vivo animal studies for IK-930 typically involve xenograft tumor models in mice. Mice bearing subcutaneous tumors derived from cancer cell lines with YAP/TAZ-TEAD dependency are treated with IK-930 via oral administration at various doses. Tumor growth inhibition is monitored over time, and at study endpoint, tumors are harvested for analysis of TEAD target gene expression, proliferation markers, and compound exposure levels. Pharmacokinetic parameters are also assessed in these studies.
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| ADME/Pharmacokinetics |
IK-930 demonstrates good pharmacokinetic properties in BALB/c mice, with a Cmax of 1088 ng/mL and an AUC0-last of 4581 ng·h/mL following oral administration at 10 mg/kg. The compound has a molecular weight of 424.44 and a formula of C19H19F3N4O2S. It is soluble in DMSO at 117.5 mg/mL (276.84 mM). For in vivo administration, it can be formulated in 10% DMSO + 90% Saline (<10 mg/mL) or 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline (10 mg/mL, suspension).
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| Toxicity/Toxicokinetics |
Toxicity data for IK-930 are not extensively reported. As a research compound, comprehensive toxicological evaluations have not been performed. The compound is intended for laboratory research use only and should be handled with standard safety precautions. Appropriate personal protective equipment should be worn when handling this compound. Consult the Material Safety Data Sheet for specific safety and handling information.
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| References | |
| Additional Infomation |
IK-930 is an oral, paralogous selective TEAD inhibitor.
IK-930 is a potent, orally active, and selective TEAD inhibitor (EC50 < 0.1 μM) that blocks TEAD autopalmitoylation. It shows high selectivity over a broad panel of kinases, receptors, and transporters. IK-930 demonstrates good pharmacokinetic properties in mice, with oral bioavailability and systemic exposure. The compound is being investigated as a potential therapeutic for YAP/TAZ-dependent cancers. IK-930 is not in clinical trials and has not been approved for therapeutic use. It remains a research tool for studying TEAD biology and Hippo signaling. |
| Molecular Formula |
C19H19F3N4O2S
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|---|---|
| Molecular Weight |
424.439973115921
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| Exact Mass |
424.118
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| CAS # |
2563892-44-2
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| PubChem CID |
155342988
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
632
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNS(=O)(=O)C1=CC(=C(C=C1)NCC2=CC=C(C=C2)C(F)(F)F)C3=CN(C=N3)C
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| InChi Key |
TVBGCXJDLVRDSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19F3N4O2S/c1-23-29(27,28)15-7-8-17(16(9-15)18-11-26(2)12-25-18)24-10-13-3-5-14(6-4-13)19(20,21)22/h3-9,11-12,23-24H,10H2,1-2H3
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| Chemical Name |
N-methyl-3-(1-methylimidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]methylamino]benzenesulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (235.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3560 mL | 11.7802 mL | 23.5605 mL | |
| 5 mM | 0.4712 mL | 2.3560 mL | 4.7121 mL | |
| 10 mM | 0.2356 mL | 1.1780 mL | 2.3560 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT05228015
Conditions:Solid Tumors, Adult|Solid Tumor|Malignant Pleural Mesothelioma (MPM)|Epithelioid Hemangioendothelioma (EHE)|NF2 Deficient Mesothelioma|Other NF2 Deficient Solid Tumors and Solid Tumors with YAP1/TAZ Fusion Genes|NF2 Deficiency|YAP1 or TAZ Gene FusionsProducts are for research use only; We do not sell to patients
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