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Chemical Structure| 18228-17-6 Chemical Structure| 18228-17-6

Structure of KG-501
CAS No.: 18228-17-6

Chemical Structure| 18228-17-6

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KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction.

Synonyms: Naphtholas-ephosphate; 2-naphthol-AS-E-phosphate; Naphthol AS-E phosphate

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Product Details of KG-501

CAS No. :18228-17-6
Formula : C17H13ClNO5P
M.W : 377.72
SMILES Code : O=C(C1=C(OP(O)(O)=O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3
Synonyms :
Naphtholas-ephosphate; 2-naphthol-AS-E-phosphate; Naphthol AS-E phosphate
MDL No. :MFCD00042718
InChI Key :RQAQWBFHPMSXKR-UHFFFAOYSA-N
Pubchem ID :87517

Safety of KG-501

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of KG-501

epigenetics

Isoform Comparison

Biological Activity

Target
  • bromodomain

In Vitro:

Cell Line
Concentration Treated Time Description References
PC12 cells 10 µM 30 min Inhibited HJG-induced neurite outgrowth Front Pharmacol. 2017 Nov 21;8:850.
Human mesenchymal stem cells (hMSCs) 30 µM 1 hour KG-501 abrogated PTH1-34 upregulation of CYP27B1 at both 2 hours and 8 hours Aging Cell. 2011 Dec;10(6):962-71.
RAW264.7 cells 10 µM 24 hours KG-501 significantly decreased the boosting effect of curcumin on HGF expression Acta Pharmacol Sin. 2021 Mar;42(3):422-435.
CCD-18Co cells 10 µM 24 hours KG-501 significantly decreased the boosting effect of curcumin on HGF expression Acta Pharmacol Sin. 2021 Mar;42(3):422-435.
Primary microglial cells 25 µM 30 minutes KG-501 completely inhibited BAA-induced CREB phosphorylation and prodynorphin expression. Sci Rep. 2017 Mar 22;7:45056.
HEK293T cells 10-25 µM 4 hours KG-501 inhibits CREB-dependent transcription Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7.
Huh7 cells 10 µM 48 hours Inhibited CREB1 phosphorylation and partially reversed TUFT1 overexpression-induced CREB1 nuclear translocation and lipid accumulation J Immunol Res. 2022 Jun 19;2022:1590717.
LNCaP cells 25 µM 48 hours KG-501 inhibited CREB-mediated transcriptional activation and significantly reduced Nurr1 promoter activity BMC Cancer. 2016 Mar 31;16:257.
1273/99 0.63-5 µM 72 hours Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo. Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
FUJI 0.63-5 µM 72 hours Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo. Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
SYO-I 0.63-5 µM 72 hours Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo. Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
CME-1 0.63-5 µM 72 hours Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo. Cell Oncol (Dordr). 2022 Jun;45(3):399-413.
HS-SY-II 0.63-5 µM 72 hours Inhibition of CREB activity reduces downstream target expression, accompanied by suppression of SySa cell proliferation and induction of apoptosis in vitro and in vivo. Cell Oncol (Dordr). 2022 Jun;45(3):399-413.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Neuropathic pain model Intrathecal injection 10 μg Single injection KG-501 completely inhibited BAA-induced mechanical antiallodynia. Sci Rep. 2017 Mar 22;7:45056.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.24mL

2.65mL

1.32mL

26.47mL

5.29mL

2.65mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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