2. PROTAC Neuronal Signaling Epigenetics Cell Cycle/DNA Damage Apoptosis Immunology/Inflammation Autophagy
  3. PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK
  4. DB0614

DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))

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DB0614

DB0614 Chemische Struktur

CAS. Nr. : 2769753-47-9

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DB0614 Related Antibodies

Top Publications Citing Use of Products

Alle PROTACs Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
Aurora Kinase Aurora A Aurora B Aurora C

Alle CaMK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
CaMK II CaMK III/eEF-2K CAMK IV PHK Trio DCAMKL

Alle CDK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
SIK1 SIK2 SIK3

Alle LIM Kinase (LIMK) Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
LIMK1 LIMK2

Alle ULK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
ULK1 ULK2

  • Biologische Aktivität

  • Reinheit & Dokumentation

  • Verweise

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Beschreibung

DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity[1][2].(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))

IC50 & Target

CDK6

 

CDK16/Cyclin Y

 

ULK1

 

Aurora Kinase

 

SIK2

 

LIMK2

 

In Vitro

DB0614 (1 μM, 5 h) is E3-ligase dependent on the degradation of the protein mitosis A-related kinase 9 (NEK9) in Cereblon (CRBN)-/- MOLT-4 cells[1].
DB0614 (1 μM, 6 h) shows high levels of degradation but not full loss in NEK9 which is dependent on the proteasome, neddylation, E1 inhibition and CRBN binding in HCT116 cells[2].

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

DB0614 Related Antibodies

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 0-10000 nM
Incubation Time: 5 h
Result: Degradated the protein NEK9 maximamly at 125 nM in MOLT4 cells.

Western Blot Analysis[2]

Cell Line: HCT116 cells
Concentration: 0-10 μM
Incubation Time: 6 h
Result: Showed high levels of degradation but not full loss in NEK9 levels in HCT116 cells.
Molekulargewicht

822.95

Formel

C41H42N8O7S2
CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C(N1C3C(NC(CC3)=O)=O)=O)C(OCCCCCN4CCN(CC4)C5=CC=C(NC6=NC7=C(SC=C7C8=CC(NS(=O)(C)=O)=CC=C8)C=N6)C=C5)=CC=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 2.78 mg/mL (3.38 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 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 1.2151 mL 6.0757 mL 12.1514 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

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Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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. 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 1.2151 mL 6.0757 mL 12.1514 mL 30.3785 mL
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DB0614 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:

DB06142769753-47-9DB 0614DB-0614PROTACsAAK1Aurora KinaseCaMKCDKFerroptosisSalt-inducible Kinase (SIK)LIM Kinase (LIMK)ULKAdaptor-associated Kinase 1AP2-associated kinase 1Calmodulin-dependent protein kinasesCalmodulin-dependent kinasesCyclin dependent kinaseLIMKsUnc-51 like kinasePROTACNEK9 inhibitorCereblon ligandthienopyrimidine scaffoldaberrant kinase activityInhibitorinhibitorinhibit

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