2. PROTAC Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  3. PROTACs CCR E1/E2/E3 Enzyme
  4. PROTAC CCR9 Degrader 1

PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.
(Pink: CCR9 ligand (HY-15724); Blue: VHL ligand (HY-125845); Black: linker (HY-W016735)).

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

PROTAC CCR9 Degrader 1

PROTAC CCR9 Degrader 1 Chemical Structure

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PROTAC CCR9 Degrader 1 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease[1][2]. (Pink: CCR9 ligand (HY-15724); Blue: VHL ligand (HY-125845); Black: linker (HY-W016735)).

IC50 & Target

CCR9

78.0 nM (Ki)

VHL

 

In Vitro

PROTAC CCR9 Degrader 1 (compound 13) binds to the intracellular allosteric binding site (IABS) of CCR9 in live HEK293T cells, with a Ki value of 151 nM[1].
PROTAC CCR9 Degrader 1 (0.1-10000 nM) induces concentration-dependent degradation of cell surface CCR9 in HEK293T cells, reaching DCmax at 10 nM, with a hook effect occurring at concentrations >10 nM[1].
PROTAC CCR9 Degrader 1 exhibits selectivity for CCR9 over CCR2 and CCR7, with no cytotoxicity[1].
PROTAC CCR9 Degrader 1 (the PROTAC shown in Figure 8) moderately degrades CCR9 in cell-based assays, and exhibits excellent selectivity over CCR2 and CCR7[2].

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

PROTAC CCR9 Degrader 1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 0.1, 1, 10, 25, 100, 500, 1000, 2500 nM
Incubation Time: 48 h
Result: Showed no cytotoxicity in cells.
Selectively induced a reduction in CCR9
levels, without affecting the levels of the related chemokine receptors CCR2 and CCR7.
Molecular Weight

1144.75

Formula

C55H66ClN9O12S2
SMILES

CC(N=CS1)=C1C(C=C2)=CC=C2CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(COCC4=CN=NN4CCOCCOCCOC5=[N+]([O-])C=CC(C(C6=CC(Cl)=CC=C6NS(C7=CC=C(C(C)(C)C)C=C7)(=O)=O)=O)=C5)=O)C(C)(C)C)=O)=O
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
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PROTAC CCR9 Degrader 1 Related Classifications

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The molarity calculator equation

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

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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:

PROTAC CCR9 Degrader 1PROTACsCCRE1/E2/E3 EnzymeCC chemokine receptorE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseintracellular allosteric binding siteCCR2Crohn's diseaseproteasomal degradationubiquitinationVHL E3 ligaseHEK293T cellsGPCRCCR9CCR7Inhibitorinhibitorinhibit

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