Product Name :
KG-501
Description:
KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
CAS:
18228-17-6
Molecular Weight:
377.72
Formula:
C17H13ClNO5P
Chemical Name:
({3-[(4-chlorophenyl)carbamoyl]naphthalen-2-yl}oxy)phosphonic acid
Smiles :
OP(O)(=O)OC1C=C2C=CC=CC2=CC=1C(=O)NC1C=CC(Cl)=CC=1
InChiKey:
RQAQWBFHPMSXKR-UHFFFAOYSA-N
InChi :
InChI=1S/C17H13ClNO5P/c18-13-5-7-14(8-6-13)19-17(20)15-9-11-3-1-2-4-12(11)10-16(15)24-25(21,22)23/h1-10H,(H,19,20)(H2,21,22,23)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.|Product information|CAS Number: 18228-17-6|Molecular Weight: 377.72|Formula: C17H13ClNO5P|Chemical Name: ({3-[(4-chlorophenyl)carbamoyl]naphthalen-2-yl}oxy)phosphonic acid|Smiles: OP(O)(=O)OC1C=C2C=CC=CC2=CC=1C(=O)NC1C=CC(Cl)=CC=1|InChiKey: RQAQWBFHPMSXKR-UHFFFAOYSA-N|InChi: InChI=1S/C17H13ClNO5P/c18-13-5-7-14(8-6-13)19-17(20)15-9-11-3-1-2-4-12(11)10-16(15)24-25(21,22)23/h1-10H,(H,19,20)(H2,21,22,23)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 6 mg/mL (15.{{Sulindac} medchemexpress|{Sulindac} Immunology/Inflammation|{Sulindac} Biological Activity|{Sulindac} Data Sheet|{Sulindac} supplier|{Sulindac} Epigenetics} 88 mM; Need ultrasonic and warming).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Methoxsalen} web|{Methoxsalen} Metabolic Enzyme/Protease|{Methoxsalen} Protocol|{Methoxsalen} Formula|{Methoxsalen} supplier|{Methoxsalen} Cancer} |Shelf Life: ≥12 months if stored properly.PMID:34856019 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|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. 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. 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.|Products are for research use only. Not for human use.|
