country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-158152

Copy Link Print Information

CRBNL-Biguanide PROTAC 1

CRBNL-Biguanide PROTAC 1 is a Biguanide-PROTAC that recruits Cereblon and an AMPK activator, composed of CRBNL, a hydrophobic linker, and a PEB-Biguanide moiety. The degradation mechanism of CRBNL-Biguanide PROTAC 1 is hypothesized to involve PEB-Biguanide promoting mitochondrial enrichment and activating AMPK, while simultaneously recruiting Cereblon to bring it into proximity with mitochondrial proteins, thereby reducing COXII and NDUFB8 protein levels and perturbing mitochondrial oxidative phosphorylation. CRBNL-Biguanide PROTAC 1 is useful for pancreatic cancer and mitochondrial protein regulation research.
(Pink: AMPK ligand (HY-121006); Blue: Cereblon ligand (HY-103597); Black: linker).

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

Formula: C₃₃H₃₀N₈O₈
Molecular Weight:666.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

CRBNL-Biguanide PROTAC 1 Chemical Structure

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

CRBNL-Biguanide PROTAC 1 is a Biguanide-PROTAC that recruits Cereblon and an AMPK activator, composed of CRBNL, a hydrophobic linker, and a PEB-Biguanide moiety. The degradation mechanism of CRBNL-Biguanide PROTAC 1 is hypothesized to involve PEB-Biguanide promoting mitochondrial enrichment and activating AMPK, while simultaneously recruiting Cereblon to bring it into proximity with mitochondrial proteins, thereby reducing COXII and NDUFB8 protein levels and perturbing mitochondrial oxidative phosphorylation. CRBNL-Biguanide PROTAC 1 is useful for pancreatic cancer and mitochondrial protein regulation research^[1]. (Pink: AMPK ligand (HY-121006); Blue: Cereblon ligand (HY-103597); Black: linker).

All PROTACs Isoforms :

All AMPK Isoforms :

All COX Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KP-4	EC50	0.15 mM	Antiproliferative activity against human KP4 pancreatic cancer cells assessed as half maximal concentration affecting growth and viability incubated for 72 hrs. Antiproliferative activity against human KP4 pancreatic cancer cells assessed as half maximal concentration affecting growth and viability incubated for 72 hrs.	2024.03.17.585436

In Vitro

Anti-cancerMitochondrial FunctionMitochondrial Oxidative Phosphorylation

Anti-cancer

CRBNL-Biguanide PROTAC 1 (compound 12) (72 h) inhibits the growth and viability of KP4 pancreatic cancer cells with an EC₅₀ of 0.15 mM^[1].

Mitochondrial Function

Mitochondrial Oxidative Phosphorylation

CRBNL-Biguanide PROTAC 1 (500 μM; 24 h) promotes AMPK phosphorylation and decreases mitochondrial OXPHOS protein levels, primarily involving complexes I and IV in KP4 cells^[1].
CRBNL-Biguanide PROTAC 1 (5-500 μM; 24 h) decreases COXII (Complex IV) and NDUFB8 (Complex I) protein levels in KP4 cells, with changes in protein levels occurring at concentrations of 250 μM and above^[1].

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

Western Blot Analysis^[1]

Cell Line:

KP4
Concentration:

5, 50, 100, 250, 500 μM
Incubation Time:

24 h
Result:

Increased AMPK phosphorylation.
Reduced mitochondrial OXPHOS protein levels, with alterations mainly involving complexes I and IV.

Western Blot Analysis^[1]

Cell Line:

KP4
Concentration:

500 μM
Incubation Time:

24 h
Result:

Reduced COXII (Complex IV) and NDUFB8 (Complex I) protein levels at concentrations of 250 μM and above.

Related Protocols :

Chemical Information

Molecular Weight 666.64
Formula C₃₃H₃₀N₈O₈
SMILES

O=CO.N=C(NC(NCC1=CC=C(C=C1)C#CC2=CC=C(C=C2)NC(COC3=CC=CC4=C3C(N(C4=O)C5CCC(NC5=O)=O)=O)=O)=N)N
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Vatté J, et al. Biguanide-PROTACs: Modulating Mitochondrial Proteins in Pancreatic Cancer Cells. bioRxiv. 2024 Mar 19.

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

CRBNL-Biguanide PROTAC 1

All PROTACs Isoforms

All AMPK Isoforms

All COX Isoforms