KG-501
Based on 23 publication(s) in Google Scholar
KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.45%
- No. CAS: 18228-17-6
- Fòrmula: C17H13ClNO5P
- Peso molecular:377.72
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) KG-501
More- Adv Funct Mater. 2023 Jan 20.
- Nat Commun. 2023 Sep 22;14(1):5894. [Abstract]
- J Exp Clin Cancer Res. 2024 Aug 20;43(1):233. [Abstract]
- Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]
- Cell Commun Signal. 2022 Apr 12;20(1):52. [Abstract]
- J Neuroinflammation. 2020 Jan 10;17(1):13. [Abstract]
- Small Methods. 2022 Mar;6(3):e2100763. [Abstract]
- Brain Behav Immun. 2024 Jul:119:36-50. [Abstract]
- J Ethnopharmacol. 2026 May 10:362:121259. [Abstract]
- Ecotoxicol Environ Saf. 2024 Feb:271:115989. [Abstract]
- Cell Biosci. 2023 Oct 3;13(1):186. [Abstract]
- Int Immunopharmacol. 2021 Sep:98:107689. [Abstract]
- Environ Toxicol Pharmacol. 2024 Mar:106:104393. [Abstract]
- iScience. 2025 Nov 17;28(12):114098. [Abstract]
- Korean J Pain. 2023 Jul 1;36(3):335-346. [Abstract]
- Toxicol Appl Pharmacol. 2022 Apr 15:441:115969. [Abstract]
- J Alzheimers Dis. 2022;85(1):167-178. [Abstract]
- Photochem Photobiol. 2024 Jan-Feb;100(1):214-224. [Abstract]
- Biochem Biophys Res Commun. 2026 Feb 26:802:153329. [Abstract]
- Res Sq. 2024 Oct 10.
- Biomed Pharmacother. 2023 Jan:157:114054. [Abstract]
- Research Square Preprint. 2021 Feb.
- Research Square Preprint. 2021 Feb.
Customer Validation & Images
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Bio/Physico-chemical Assay
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RT-PCR
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IF
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Cell Imaging/Staining
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Flow Cytometry
Actividad biológica
IC50: 6.89 μM (CREB)[1].
KG-501, which directly targets the KIX domain of CBP, results in a disrupted CREB-CBP complex, inhibits CREB-target gene induction, and inhibits IL-1β-mediated angiogenic activity in NSCLC[1]. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity[2]. KG-501 can also inhibit NF-κB transcription activity because NF-κB also uses CBP as a cofactor to regulate gene expression. The migration of HUVECs induced by CM from A549 cells treated with IL-1β plus 10 μM of KG-501 is significantly lower than that induced by CM from A549 cells treated with IL-1β alone. At 10 μM, KG-501 suppresses the expression of all of the IL-1β–induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β–induced CXCL5 protein secretion. Similar effects of KG-501 are also observed in the H1734 cell line[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 18228-17-6
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Appearance Solid
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Peso molecular 377.72
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Fòrmula C17H13ClNO5P
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Color White to light yellow
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SMILES
O=C(C1=C(OP(O)(O)=O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3
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Synonyms
Naphthol AS-E phosphate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (23)
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Journal Impact Factor
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Most Recent
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Nat Commun
CREB1-driven CXCR4hi neutrophils promote skin inflammation in mouse models and human patients. [Abstract]2023 Sep 22;14(1):5894. PMID: 37736772 -
J Exp Clin Cancer Res
Areca nut-induced metabolic reprogramming and M2 differentiation promote OPMD malignant transformation. [Abstract]2024 Aug 20;43(1):233. PMID: 39160581
KG-501 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Aug 20;43(1):233. [Abstract]
KG-501 (300 μM; 1 h) suppressed surface expression of CXCR4, maturation/activation marker including CD10, CD101, degranulation marker CD63 in CXCR4hi neutrophils.
KG-501 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Aug 20;43(1):233. [Abstract]
Representative co-staining of DNA (Hoechst), Cit-H3 (citrullinated histone-3, red), and MPO (myeloperoxidase, green) to assess NETs formation in psoriatic neutrophils in vitro after pretreatment with KG-501 (300 μM) for 1 h. Scale bar = 20 µm
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Environ Sci Technol
Placentation Disruption by Perfluorooctanoic Acid and Perfluorooctanesulfonate in Human Trophoblast Organoids. [Abstract]2025 Sep 30;59(38):20263-20275. PMID: 40954114
KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]
KG-501 (156.25, 312.5, 625, 1250, 2500, 5000, 10000 nM) inhibited CREB transcriptional activity, as measured by a dual-luciferase reporter assay in HEK-293T cells.
KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]
KG-501 (500 nM; 7 days) decreased the CYP19A1 mRNA expression in human trophoblast organoids.
KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]
KG-501 (500 nM; 7 days) decreased the STB marker SDC-1 in human trophoblast organoids.
KG-501 purchased from MedChemExpress. Usage Cited in: Environ Sci Technol. 2025 Sep 30;59(38):20263-20275. [Abstract]
Representative images of the fusion assay of trophoblast organoids stained for F-actin and DAPI treated with KG-501 (500 nM; 7 days).
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Cell Commun Signal
Receptor activity-modifying protein 1 regulates mouse skin fibroblast proliferation via the Gαi3-PKA-CREB-YAP axis. [Abstract]2022 Apr 12;20(1):52. PMID: 35413847 -
J Neuroinflammation
Isotalatizidine, a C19-diterpenoid alkaloid, attenuates chronic neuropathic pain through stimulating ERK/CREB signaling pathway-mediated microglial dynorphin A expression. [Abstract]2020 Jan 10;17(1):13. PMID: 31924228 -
Small Methods
Sympathetic Neurostress Drives Osteoblastic Exosomal MiR-21 Transfer to Disrupt Bone Homeostasis and Promote Osteopenia. [Abstract]2022 Mar;6(3):e2100763. PMID: 35312228 -
Brain Behav Immun
Dexamethasone attenuates neuropathic pain through spinal microglial expression of dynorphin A via the cAMP/PKA/p38 MAPK/CREB signaling pathway. [Abstract]2024 Jul:119:36-50. PMID: 38555991 -
J Ethnopharmacol
Epimedium brevicornum Maxim and Ligustrum lucidum Ait enhance glucocorticoid-associated anti-inflammatory effects in asthma via the cAMP/PKA/CREB signaling pathway. [Abstract]2026 May 10:362:121259. PMID: 41690429 -
Ecotoxicol Environ Saf
Proteomic analysis reveals that cigarette smoke exposure diminishes ovarian reserve in mice by disrupting the CREB1-mediated ovarian granulosa cell proliferation-apoptosis balance. [Abstract]2024 Feb:271:115989. PMID: 38242047 -
Cell Biosci
Gut microbial metabolite deoxycholic acid facilitates Th17 differentiation through modulating cholesterol biosynthesis and participates in high-fat diet-associated colonic inflammation. [Abstract]2023 Oct 3;13(1):186. PMID: 37789469 -
Int Immunopharmacol
The ERK/CREB/PTN/syndecan-3 pathway involves in heparin-mediated neuro-protection and neuro-regeneration against cerebral ischemia-reperfusion injury following cardiac arrest. [Abstract]2021 Sep:98:107689. PMID: 34153666 -
Environ Toxicol Pharmacol
2024 Mar:106:104393. PMID: 38367920 -
iScience
TLR9 decreases FOXO3 expression to prevent excessive inflammation in macrophage activation syndrome. [Abstract]2025 Nov 17;28(12):114098. PMID: 41438053 -
Korean J Pain
Perampanel ameliorates nitroglycerin-induced migraine through inhibition of the cAMP/PKA/CREB signaling pathway in the trigeminal ganglion in rats. [Abstract]2023 Jul 1;36(3):335-346. PMID: 37394274 -
Toxicol Appl Pharmacol
Icariin promotes mouse Leydig cell testosterone synthesis via the Esr1/Src/Akt/Creb/Sf-1 pathway. [Abstract]2022 Apr 15:441:115969. PMID: 35259346 -
J Alzheimers Dis
Astrocytic N-Methyl-D-Aspartate Receptors Protect the Hippocampal Neurons Against Amyloid-β142-Induced Synaptotoxicity by Regulating Nerve Growth Factor. [Abstract]2022;85(1):167-178. PMID: 34776441 -
Photochem Photobiol
Photobiomodulation therapy at 632 nm wavelength ameliorates intrauterine adhesion via activation of cAMP/PKA/CREB pathway. [Abstract]2024 Jan-Feb;100(1):214-224. PMID: 37212452 -
Biochem Biophys Res Commun
GALNT3-mediated AKT1 glycosylation activates the AKT1/CREB signaling pathway to inhibit high glucose-induced spermatogenic cell apoptosis and mitochondrial dysfunction. [Abstract]2026 Feb 26:802:153329. PMID: 41592399 -
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Biomed Pharmacother
Cordycepin improved neuronal synaptic plasticity through CREB-induced NGF upregulation driven by MG-M2 polarization: a microglia-neuron symphony in AD. [Abstract]2023 Jan:157:114054. PMID: 36462314 -
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Solvente y solubilidad
DMSO : 6 mg/mL (15.88 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.29 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lee JW, et al. A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress. PLoS One. 2015 Apr 21;10(4):e0122628. [Content Brief]
[2]. Best JL et al. Identification of small-molecule antagonists that inhibit an activator: coactivator interaction. Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7 [Content Brief]
[3]. Sun H, et al. Cyclic AMP-responsive element binding protein- and nuclear factor-kappaB-regulated CXC chemokine gene expression in lung carcinogenesis. Cancer Prev Res (Phila). 2008 Oct;1(5):316-28. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6475 mL | 13.2373 mL | 26.4746 mL | 66.1866 mL |
| 5 mM | 0.5295 mL | 2.6475 mL | 5.2949 mL | 13.2373 mL | |
| 10 mM | 0.2647 mL | 1.3237 mL | 2.6475 mL | 6.6187 mL | |
| 15 mM | 0.1765 mL | 0.8825 mL | 1.7650 mL | 4.4124 mL |
KG-501 Related Classifications
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