CHELERYTHRIN CL
Chelerythrine chloride
CAS: 3895-92-9
Molecular Formula: C21H18ClNO4
CHELERYTHRIN CL - Names and Identifiers
CHELERYTHRIN CL - Physico-chemical Properties
| Molecular Formula | C21H18ClNO4 |
| Molar Mass | 383.82 |
| Melting Point | 195-205 °C |
| Boling Point | 711.4°C at 760 mmHg |
| Solubility | DMSO : 4.35 mg/mL (11.33 mM; Need ultrasonic) |
| Appearance | Orange powder |
| Color | yellow to orange |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| MDL | MFCD00060717 |
| Physical and Chemical Properties | Orange-red powder, soluble in organic solvents such as methanol, ethanol, DMSO, etc., is derived from the fruit of Macrosin, celadus, and zanthoxylum nitidum. |
| In vitro study | Chelerythrine interacts with the catalytic domain of PKC and is a competitive inhibitor of the phosphate receptor (histone IIIS) with a Ki value of 0.7 μm and a noncompetitive inhibitor of APT. Chelerythrine exhibited potent cytotoxicity against L-1210 cells with an IC50 of 0.53 μm. Chelerythrine did not change any activity of PKA,TPK and Ca/CM-PK, and the inhibition of PKC activity by Chelerythrine did not change in different substrates, including GS,MLC,MBP and fibrinogen. Chelerythrine dose-dependently inhibited PKC activity in crude extracts of SQ-20B cells. Chelerythrine dose-dependently reduced cell activity in SCC35,JSQ3,SQ20B and SCC61 cells as measured by the MTT method. In HUVECs, chelythrine chloride (5 μm) inhibits VEGF-induced ICAM-1,VCAM-1, and E-selectin expression. Chelerythrine chloride (5 μm) inhibits VEGF-induced NF-κB activity in HUVECs. Chelerythrine chloride (5 μm) inhibits basal and VEGF-induced leukocyte adhesion aggregation in HUVECs. Chelerythrine (6 mM-30 mM) rapidly induces cell densification and contraction in cardiomyocytes, which subsequently leads to cell death. Chelerythrine(30 μm)-induced cardiomyocyte death was accompanied by nuclear lysis and caspase-3 and -9 activation in primary cultures of neonatal rat ventricular myocytes. In cardiomyocytes, chelythrine (10 μm) causes cytochrome C release from mitochondria, suggesting that ROS regulates chelythrine-induced cytochrome C release. Chelerythrine replaces the fluorescently labeled BH3 domain polypeptide from the recombinant GST-BcLXL fusion protein with an IC50 of 1.5 μm. Treatment with Chelerythrine at 2.5 μm and 5 μm for 16 hours induced a significant decrease in mitochondrial membrane potential as shown by JC-1 green fluorescence in human neuroblastoma SH-SY5Y cells. In SH-SY5Y cells, chelythrine (5 μm) also induces sub-G1 DNA appearance indicative of apoptosis. Chelerythrine (10 μm) induces changes in mitochondrial membrane potential and CytC release from mitochondria in SH-SY5Y cells. |
| In vivo study | In mice bearing SQ-20B xenografts, chelythrine (5 mg/kg I. p.) caused a delay in tumor growth. In adult rats, chelythrine (5 mg/kg) treatment significantly increased TUNEL-positive nuclei in myocardium and increased lysis of caspase-3 and -9. |
CHELERYTHRIN CL - Risk and Safety
| Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R36/37 - Irritating to eyes and respiratory system. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. S36/37 - Wear suitable protective clothing and gloves. |
| UN IDs | UN 1544PSN1 6.1 / PGII |
| WGK Germany | 3 |
| RTECS | FL9200000 |
| HS Code | 29349990 |
CHELERYTHRIN CL - Reference Information
| biological activity | chellerythrine is a potent, selective PKC antagonist with an IC50 of 0.66 μm. |
| Target | Value |
| PKC (Cell-free assay) | 0.66 μM |
| uses | The chylestrine hydrochloride can be used for the treatment of digestive tract cancer, liver cancer, ovarian cancer, lung cancer, head and neck cancer, malignant lymphoma, etc, the curative effect of gastric cancer and ovarian cancer is better. |
Last Update：2024-04-10 22:41:03
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View History
CHELERYTHRIN CL
FORMYLOXYMANDELOYL CHLORIDE
[dimethylamino(fluoro)phosphoryl]-dimethyl-amine
Α-D-吡喃葡萄糖酰氟
2-CHLORO-4-ISOPROPOXY-5-METHOXY-BENZOIC ACID
盐酸卡替洛尔
Einecs 246-623-3
TERT-BUTYLPEROXY 2-ETHYLHEXYL CARBONATE
2,4,6-TRIPHENYLPYRYLIUM TETRAFLUOROBORATE
L-Adrenalin
FORMYLOXYMANDELOYL CHLORIDE
[dimethylamino(fluoro)phosphoryl]-dimethyl-amine
Α-D-吡喃葡萄糖酰氟
2-CHLORO-4-ISOPROPOXY-5-METHOXY-BENZOIC ACID
盐酸卡替洛尔
Einecs 246-623-3
TERT-BUTYLPEROXY 2-ETHYLHEXYL CARBONATE
2,4,6-TRIPHENYLPYRYLIUM TETRAFLUOROBORATE
L-Adrenalin