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Chemical Structure| 82-08-6 Chemical Structure| 82-08-6

Structure of Rottlerin
CAS No.: 82-08-6

Chemical Structure| 82-08-6

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Rottlerin, a principal phenolic compound isolated and purified from Kamala plant Mallotus philippinensis, exers its tumour-suppressive function in ACC.

Synonyms: Mallotoxin; NSC 94525; Kamalin

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Product Details of Rottlerin

CAS No. :82-08-6
Formula : C30H28O8
M.W : 516.54
SMILES Code : O=C(C1=C(O)C(CC2=C(O)C(C)=C(O)C(C(C)=O)=C2O)=C(O)C3=C1OC(C)(C)C=C3)/C=C/C4=CC=CC=C4
Synonyms :
Mallotoxin; NSC 94525; Kamalin
MDL No. :MFCD00017361
InChI Key :DEZFNHCVIZBHBI-ZHACJKMWSA-N
Pubchem ID :5281847

Safety of Rottlerin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335-H302+H312+H332
Precautionary Statements:P264-P302+P352-P304+P340-P305+P351+P338-P332+P313-P337+P313

Related Pathways of Rottlerin

epigenetics

Isoform Comparison

Biological Activity

Description
Rottlerin is a compound extracted from Mallotus Philippinensis, functions as a selective inhibitor of Protein Kinase C (PKC), demonstrating IC50 values of 3-6 μM for PKCδ, 30-42 μM for PKCα,β,γ, and 80-100 μM for PKCε,η,ζ. Its mode of action includes acting as a direct mitochondrial uncoupler and promoting autophagy by acting on a signaling cascade upstream of mTORC1. Furthermore, Rottlerin triggers apoptosis through the activation of caspase 3[1].[2].[3].

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat cardiac myocytes 1 μM 3 h Rottlerin completely rescued the contractile deficits in myocytes PMC3358121
SW620 1-2 μM 20 h Rottlerin effectively decreased the B7-H4 protein level. PMC8996430
HCT116 1-2 μM 20 h Rottlerin effectively decreased the B7-H4 protein level. PMC8996430
Rat brain astrocytes (RBA) 1 μM 1 h To evaluate the effect of Rottlerin on PMA-induced MMP-9 expression, the results showed that Rottlerin significantly inhibited PMA-induced MMP-9 expression. PMC7276071
HK-2 cells 1 μM 48 h To investigate the effect of Rottlerin on hypoxia-induced fibrotic and inflammatory responses in HK-2 cells, results showed that Rottlerin significantly inhibited the activation of the cGAS-STING signaling pathway and alleviated fibrosis and inflammation. PMC11228024
Human umbilical vein endothelial cells (HUVECs) 5 μM 48 h Rottlerin ameliorates high glucose-induced apoptosis in HUVECs by inhibiting PKC δ, reducing the expression of cleaved-caspase 3, and decreasing the percentage of TUNEL-positive cells. PMC11137154

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Langendorff-perfused isolated heart model Supplied in the cardioplegia 1 μM 1 minute every 30 minutes for 2 hours Rottlerin significantly improved cardiac function and coronary perfusion following cardioplegic arrest PMC3358121
C57BL/6N mice Trimethyltin (TMT)-induced dentate gyrus injury model Intraperitoneal injection 5 mg/kg Every 12 hours for 5 times, lasting 3-5 days To investigate the effect of Rottlerin on TMT-induced astrocyte polarization, results showed that Rottlerin significantly decreased Iba-1 and C3 expression, indicating that PKCδ inhibition attenuates microglial activation and A1 astrocyte phenotype polarization. PMC9188234
BALB/c nude mice HCT116 tumor model Oral 20 mg/kg Once every two days for 54 days Rottlerin significantly reduced lung metastasis. PMC8996430
Mice Unilateral ureteral ligation (UUO) model Intraperitoneal injection 10 mg/kg Daily for 13 days To investigate the effect of Rottlerin on UUO-induced kidney fibrosis in mice, results showed that Rottlerin significantly alleviated kidney fibrosis, inflammation, and activation of the cGAS-STING signaling pathway. PMC11228024

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.68mL

1.94mL

0.97mL

19.36mL

3.87mL

1.94mL

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