2. Metabolic Enzyme/Protease
  3. MMP
  4. cyclo(RLsKDK)

cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer.

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

Custom Peptide Synthesis

cyclo(RLsKDK) Chemical Structure

cyclo(RLsKDK) Chemical Structure

CAS No. : 1975145-82-4

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Based on 1 publication(s) in Google Scholar

Other Forms of cyclo(RLsKDK):

cyclo(RLsKDK) Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE cyclo(RLsKDK)

View All MMP Isoform Specific Products:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer[1].

Cellular Effect
Cell Line Type Value Description References
COS-7 IC50
182 nM
Compound: 1
Inhibition of recombinant ADAM8 (unknown origin) expressed in African green monkey COS7 cells co-expressing CD23 assessed as inhibition of CD23 shedding after 24 hrs by ELISA
Inhibition of recombinant ADAM8 (unknown origin) expressed in African green monkey COS7 cells co-expressing CD23 assessed as inhibition of CD23 shedding after 24 hrs by ELISA
[PMID: 27407033]
In Vitro

cyclo(RLsKDK) promotes ADAM8 activation and CD23 shedding with IC50 values of 120 nM and 182 nM, respectively[2].
cyclo(RLsKDK) (200 nM; 0-120 h) increases activity of pro-ADAM8[2].
cyclo(RLsKDK) (200 nM and 500 nM; 12 h) promotes the growth of Panc1_ctrl and Panc1_A8 cells[2].
cyclo(RLsKDK) (500 nM) causes ERK1/2 phosphorylation in Panc1_ctrl and Panc1_A8 cells[2].

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

cyclo(RLsKDK) Related Antibodies

Cell Invasion Assay[2]

Cell Line: Panc1_A8 cells.
Concentration: 10, 100 and 1,000 nM.
Incubation Time: 6 h.
Result: Reduced cell invasion with dose-dependent manner.
In Vivo

cyclo(RLsKDK) (10 µg/g; i.p.; once weekly for 4 weeks) significantly reduces tumour load in mice which implant Panc1_ctrl or Panc1_A8 cells. cyclo(RLsKDK) improves the survival rate of pancreatic ductal adenocarcinoma (PDAC) mice, reduces soluble ADAM8 (sADAM8) content, pERK1/2 activation, and PDAC metastasis in the liver and lungs of PDAC mice[2].

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

727.85

Formula

C31H57N11O9
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Cyclo(Arg-Leu-{d-Ser}-Lys-Asp-Lys)
Sequence Shortening

Cyclo(RL-{d-Ser}-KDK)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (4.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3739 mL 6.8695 mL 13.7391 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3739 mL 6.8695 mL 13.7391 mL 34.3477 mL
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cyclo(RLsKDK) Related Classifications

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:

cyclo(RLsKDK)1975145-82-4BK-1361BK1361BK 1361MMPMatrix metalloproteinasesPancreatic ductal adenocarcinomaPDACPDAC micePanc1_ctrl cellsPanc1_A8 cellsADAM8ERK1/2Inhibitorinhibitorinhibit

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