| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
NSC-694623 targets histone acetyltransferases (HATs), specifically the p300/CBP-associated factor (PCAF). PCAF is a transcriptional coactivator that acetylates histones and other proteins, playing a critical role in gene expression regulation. By inhibiting PCAF, NSC-694623 modulates the acetylation of histones and transcription factors, which can affect cell proliferation and survival. This mechanism makes it a valuable tool for studying the role of HATs in cancer biology.
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| ln Vitro |
NSC 694623 inhibits HCT116 by 21% at 25 μM and shows anti-proliferative action against SK-N-SH with an IC50 of 8.93 μM [1].
In vitro, NSC-694623 is a potent HAT inhibitor with an IC50 of 15.9 µM against recombinant PCAF. It shows antiproliferative activity in cancer cell lines, with an IC50 of 8.93 µM against SK-N-SH cells and 21% inhibition in HCT116 cells at 25 µM. These data demonstrate its potential as an anti-cancer agent. The compound is soluble in DMSO at 125 mg/mL and is provided as a solid for biochemical and cell-based studies. |
| ln Vivo |
Specific in vivo activity data for NSC-694623 are not provided in the available sources. As a HAT inhibitor with in vitro anticancer activity, it would be expected to have effects in animal models of cancer. However, no specific in vivo studies, dosing regimens, or efficacy data are described. The compound is primarily utilized as a research tool for in vitro epigenetic studies.
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| Enzyme Assay |
A cell-free assay for NSC-694623 involves measuring its inhibition of PCAF enzymatic activity. In these assays, recombinant PCAF is incubated with a histone substrate and acetyl-CoA in the presence of varying concentrations of the compound. The incorporation of acetyl groups into the substrate is measured, and IC50 values are calculated. For NSC-694623, the IC50 against PCAF is 15.9 µM.
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| Cell Assay |
Cellular assays for NSC-694623 typically involve assessing its antiproliferative effects on cancer cell lines. Cells such as SK-N-SH and HCT116 are treated with varying concentrations of the compound, and cell viability is measured using standard assays. For NSC-694623, an IC50 of 8.93 µM was observed in SK-N-SH cells, and 21% inhibition was observed in HCT116 cells at 25 µM. These assays confirm its activity in a cellular context.
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| Animal Protocol |
In vivo animal experiments for NSC-694623 are not described in the available sources. As a research compound with HAT inhibitory activity, it could be evaluated in tumor xenograft models to assess its antitumor efficacy. However, no specific protocols or data are provided.
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| ADME/Pharmacokinetics |
NSC-694623 has a molecular formula of C16H16N2OS and a molecular weight of 284.38. It is soluble in DMSO at 125 mg/mL. For storage, the powder should be kept at -20°C. The compound is provided as a solid with a purity of 99.5%. Specific pharmacokinetic parameters are not reported in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for NSC-694623 are not provided in the available sources. As with many research compounds, detailed toxicological profiles are typically established during later stages of drug development. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
NSC-694623 (CAS: 907957-34-0) is a potent HAT inhibitor with an IC50 of 15.9 µM against PCAF. It exhibits antiproliferative activity in cancer cell lines, including SK-N-SH (IC50 = 8.93 µM) and HCT116 (21% inhibition at 25 µM). Its molecular formula is C16H16N2OS and its molecular weight is 284.38. The compound is used for anti-cancer research. It is not an approved drug and is strictly for research purposes.
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| Molecular Formula |
C16H16N2OS
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|---|---|
| Molecular Weight |
284.376042366028
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| Exact Mass |
284.098
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| CAS # |
907957-34-0
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| PubChem CID |
393169
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
341
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C2C=CC(CCCC)=CC=2)SC2C1=CC=CN=2
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| InChi Key |
XNGPPEMGIZDPGJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16N2OS/c1-2-3-5-12-7-9-13(10-8-12)18-16(19)14-6-4-11-17-15(14)20-18/h4,6-11H,2-3,5H2,1H3
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| Chemical Name |
2-(4-butylphenyl)-[1,2]thiazolo[5,4-b]pyridin-3-one
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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 : ~125 mg/mL (~439.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.31 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 20.8 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: ≥ 2.08 mg/mL (7.31 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 20.8 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 | 3.5164 mL | 17.5821 mL | 35.1642 mL | |
| 5 mM | 0.7033 mL | 3.5164 mL | 7.0328 mL | |
| 10 mM | 0.3516 mL | 1.7582 mL | 3.5164 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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