2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. Cbl-b-IN-16

Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity.

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

Cbl-b-IN-16 Chemical Structure

Cbl-b-IN-16 Chemical Structure

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Cbl-b-IN-16 Related Antibodies

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Description

Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity[1].

IC50 & Target

IC50: Cbl-b (30 nM)[1]
In Vitro

Cbl-b-IN-16 regulates the TCR signaling through inihibiting the autoubiquitination of Cbl-b and the ubiquitin transfer to Zap-70, with IC50s of 63 nM and 84 nM, respectively[1].
Cbl-b-IN-16 (5 μM, 20 min) inhibits the phosphorylation of Cbl-b via spleen tyrosine kinase (SYK)[1].
Cbl-b-IN-16 inhibition enhances the TCR signaling and thereby upregulates the levels of pPLCγ1 in Hu-T-cells with an EC50 of 0.61 μM[1].

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

Cbl-b-IN-16 Related Antibodies
In Vivo

Cbl-b-IN-16 reveals a pharmacokinetic profils in CD1 mice and Wistar Han rats[1]:

Pharmacokinetic Analysis of Cbl-b-IN-16 in CD1 mice and Wistar Han rats[1]

species route Dose (mg/kg) CL (mL/min/kg) Vss (L/kg) T1/2 (h) Cmax (μg/mL) Tmax (h) AUCinf (μg·h/mL) F (%) Calculated EHc
mouse iv 0.5 100 1.3 0.3 - - - - 0.66
mouse po 1.0 - - - 0.035 0.083 0.030 19 -
rat iv 0.5 55 1.6 0.45 - - - - 0.76
rat po 1.0 - - - 0.021 0.75 0.046 15 -

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

496.53

Formula

C26H27F3N6O
SMILES

O=C1C(C2=CC=CC([C@@]3(C4=NN=CN4C)C[C@H](C)C3)=C2)=CC(C(F)(F)F)=CN1[C@H](C5=CN(C)N=C5)C
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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Cbl-b-IN-16 Related Classifications

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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:

Cbl-b-IN-16E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCbl-bubiquitinationIL-2T-cellsZap-70TCR-signalingPLCγInhibitorinhibitorinhibit

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Cbl-b-IN-16
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