2. Apoptosis TGF-beta/Smad Epigenetics
  3. Apoptosis PKC
  4. Evo312

Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model.

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

Evo312 Chemical Structure

Evo312 Chemical Structure

CAS No. : 2820245-53-0

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Evo312 Related Antibodies

Top Publications Citing Use of Products

View All PKC Isoform Specific Products:

View All Isoforms
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model[1].

IC50 & Target

PKC-βI

117.34 nM (IC50)

In Vitro

Evo312 (0-160 nM, 24 h) inhibits PKCβ1 protein expression and downstream target protein phosphorylation in PANC-GR cells[1].
Evo312 (0-160 nM, 24 h) induces G2/M cell cycle arrest in PANC-GR cells, inhibiting to cell mitosis[1].
Evo312 (0-160 nM, 48 h) induces apoptosis in PANC-GR cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Evo312 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: PANC-GR (an acquired gemcitabine-resistant PC cell line, cell line PANC-GR was established in vitro from PANC-1 cells by exposing gemcitabine with gradually increasing concentrations (0.1−2 μM))
Concentration: 0, 40, 80, 160 nM
Incubation Time: 24 h
Result: Increased the number of G2/M cells from 37.53% to 58.51%, leading to mitosis.

Apoptosis Analysis[1]

Cell Line: PANC-GR, PANC-1
Concentration: 40, 80, 160 nM
Incubation Time: 48 h
Result: Increased total cell death (including early apoptosis, late apoptosis and necrosis) by 15.83%, 20.63% and 24.95%.

Western Blot Analysis[1]

Cell Line: PANC-GR, PANC-1
Concentration: 0, 40, 80, 160 nM
Incubation Time: 24 h; 48 h
Result: Inhibited the expression of PKCβ1 protein at 24 h, and inhibited the phosphorylation of glycogen synthase kinase 3β (GSK3β), protein kinase B (Akt), signal transducer and activator of transcription 5 (STAT5), and ribosomal protein S6 kinase β-1 (70S6K) in a dose-dependent manner.
Downregulated the expression levels of CDK (CDK2 and cdc2) and cyclin D1 proteins at 24 h, while upregulated the expression levels of cyclin B1 and p27 proteins.
Increased the expression levels of apoptosis markers caspase3, caspase8, and caspase9 proteins at 48 h.
In Vivo

Evo312 (5 mg/kg, ip., three times a week, 20 days) inhibits tumor growth in the PANC-GR (Gemcitabine-resistant cells) mouse xenograft model by inhibiting PKCβⅠ, whereas gemcitabine treatment resulted in negligible inhibitory effects on tumor growth[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PANC-GR cell mouse xenograft model; PANC-1 cell mouse xenograft model[1]
Dosage: 40 mg/kg; 5 mg/kg, three times a week, 20 days
Administration: Intraperitoneal injection (i.p.)
Result: Did not cause mouse death or significant toxicity at a dose of 40 mg/kg. At a dose of 5 mg/kg, the tumor volume was inhibited by 72%, and the tumor weight was reduced by 44.89% compared with the drug-loaded treatment group, with no significant toxicity or weight changes, and the expression of PKCβI in tumor tissues implanted with PANC-GR cells was effectively inhibited.
Molecular Weight

361.39

Formula

C21H19N3O3
CAS No.
SMILES

O=C1C2=C(N(C3N1CCC4=C3NC5=CC=C(OC(C)=O)C=C45)C)C=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Evo312 Related Classifications

  • 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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Evo3122820245-53-0Evo 312Evo-312ApoptosisPKCProtein kinase CPANC-1PANC-GRMRC-5Pancreatic cancer (PC)Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Evo312
Cat. No.:
HY-169006
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.