| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Fas
FAF1 (Fas-associated factor 1). FAF1 is a protein that interacts with the Fas receptor and mediates Fas-induced apoptosis. KR-33494 inhibits Fas-mediated cell death by targeting FAF1. The compound is a FAF1 inhibitor. |
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| ln Vitro |
KR-33494 is a potent inhibitor of Fas-mediated cell death. As a fluorescent-tagged and biotin-tagged probe, it enables detection and study of FAF1 interactions. Detailed IC50 values for FAF1 inhibition have not been extensively reported in the available literature.
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| ln Vivo |
In both sexes, body weight fluctuations were not influenced by KR-33493 at any dosage. No test article-related alterations were observed in hematology, serum chemistry, or urinalysis in any treatment group, regardless of gender, in rats given KR-33493 for four weeks. During a two-week period, dogs administered KR-33493 showed significantly increased male red blood cell count (RBC) values at the 1000 mg/kg/day dose compared to the control group (6.96±0.323 vs. 6.12±0.418). After the dosage period ended, red blood cell alterations did, however, reverse. The fact that there were no appreciable variations in dose-normalized AUClast among the groups suggests that linear kinetics are in charge of KR-33493 [1].
In both sexes, body weight fluctuations were not influenced by KR-33493 (a related compound) at any dosage. No detailed in vivo activity data has been published specifically for KR-33494 in the available literature. Further in vivo studies would be needed to evaluate its effects in animal models. |
| Enzyme Assay |
FAF1 binding assay: Recombinant FAF1 or cell lysates containing FAF1 are incubated with varying concentrations of KR-33494 (a fluorescent-tagged probe) in binding buffer. Binding is measured by fluorescence polarization, fluorescence resonance energy transfer (FRET), or pull-down assays using the biotin tag followed by streptavidin detection. Binding affinity and specificity are determined.
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| Cell Assay |
Fas-mediated cell death assay: Cells expressing Fas receptor are treated with KR-33494 at varying concentrations for a specified time, then stimulated with Fas ligand or agonistic anti-Fas antibody to induce apoptosis. Cell death is quantified by flow cytometry using annexin V/PI staining, caspase activity assays, or LDH release assays. The inhibition of Fas-mediated cell death is calculated.
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| Animal Protocol |
No in vivo animal experimental protocols have been published for KR-33494 in the available literature. In vivo studies would typically involve mouse models of Fas-mediated tissue injury (e.g., liver injury models), where KR-33494 would be administered via appropriate routes, followed by assessment of tissue damage, apoptosis markers, and survival.
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been published in the available literature. KR-33494 has a molecular weight of 460.34 g/mol and molecular formula C₂₀H₁₈BrN₃O₃S. It is soluble in DMSO at 92 mg/mL (199.85 mM). Comprehensive PK parameters remain to be characterized.
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| Toxicity/Toxicokinetics |
No toxicity data has been published in the available literature. KR-33494 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As a FAF1 inhibitor, potential effects on Fas-mediated apoptosis in normal tissues should be considered.
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| References | |
| Additional Infomation |
KR-33494 is a potent inhibitor of Fas-mediated cell death targeting FAF1 (Fas-associated factor 1). It is a fluorescent-tagged and biotin-tagged probe for studying FAF1 interactions in Fas-mediated apoptosis pathways. The compound is a research tool for apoptosis and cell death studies. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C20H18BRN3O3S
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|---|---|
| Molecular Weight |
460.3442
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| Exact Mass |
459.025
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| Elemental Analysis |
C, 52.18; H, 3.94; Br, 17.36; N, 9.13; O, 10.43; S, 6.96
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| CAS # |
1021497-97-1
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| Related CAS # |
1021497-97-1
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| PubChem CID |
25009726
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| Appearance |
White to off-white solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
525
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZRLJEHIUGYTTSZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18BrN3O3S/c21-15-6-8-16(9-7-15)28-13-18(25)22-17-12-24(23-19(17)20(26)27)11-10-14-4-2-1-3-5-14/h1-9,12H,10-11,13H2,(H,22,25)(H,26,27)
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| Chemical Name |
4-[[2-(4-bromophenyl)sulfanylacetyl]amino]-1-(2-phenylethyl)pyrazole-3-carboxylic acid
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| Synonyms |
KR 33494; KR-33494; KR33494
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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: ≥ 31 mg/mL (~67.3 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.43 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 (5.43 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 | 2.1723 mL | 10.8615 mL | 21.7231 mL | |
| 5 mM | 0.4345 mL | 2.1723 mL | 4.3446 mL | |
| 10 mM | 0.2172 mL | 1.0862 mL | 2.1723 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.
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