1. Epigenetics
    TGF-beta/Smad
    Autophagy
    Apoptosis
  2. PKC
    Autophagy
    Apoptosis
  3. Rottlerin

Rottlerin (Synonyms: Mallotoxin; NSC 56346; NSC 94525)

Cat. No.: HY-18980
Handling Instructions

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.

For research use only. We do not sell to patients.

Rottlerin Chemical Structure

Rottlerin Chemical Structure

CAS No. : 82-08-6

Size Price Stock Quantity
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 130 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products
  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[1][2][3].

IC50 & Target[1]

PKCδ

3 μM (IC50, Porcine spleen)

PKCα

30 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCγ

40 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCβ

42 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCη

82 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCζ

100 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCε

100 μM (IC50, baculovirus-infected Sf9 insect cells)

CaM kinase III

5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)

CKII

30 μM (IC50, holoenzyme expressed in E.coli)

PKA

78 μM (IC50, catalytic subunit from porcine heart)

In Vitro

Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC[2].
Rottlerin (20 μM) exhibits cell proliferation in HMVEC[2].

Western Blot Analysis[2]

Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration: 20 μM.
Incubation Time: 2, 6, 24 hours.
Result: Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h.

Cell Proliferation Assay[2]

Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration: 20 μM.
Incubation Time: 24/48 hours.
Result: Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively.
In Vivo

Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity[3].
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].

Animal Model: Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×106 cells mixed with Matrigel, 50:50 ratio) injection[3].
Dosage: 0 or 20 mg/kg.
Administration: Gavage 5 days per week, once daily, for 6 weeks.
Result: Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice.
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9360 mL 9.6798 mL 19.3596 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

516.54

Formula

C₃₀H₂₈O₈

CAS No.

82-08-6

SMILES

O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Rottlerin
Cat. No.:
HY-18980
Quantity:

Rottlerin

Cat. No.: HY-18980