HM5023507
HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research.
For research use only. We do not sell to patients.
- CAS No.: 1549766-06-4
- Formula: C21H18ClN7O2
- Molecular Weight:435.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kδ 5 nM (IC50) |
PI3Kγ 4 nM (IC50) |
p110α 590 nM (IC50) |
p110β 3960 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
0.005 μM
Compound: 26
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Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po
Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po
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[PMID: 31033293] |
| Sf21 | IC50 |
0.59 μM
Compound: 26
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Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol
Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol
|
[PMID: 31033293] |
Chemical Information
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CAS No. 1549766-06-4
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Molecular Weight 435.87
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Formula C21H18ClN7O2
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SMILES
O=C1N(C2=CC=CC=C2)C([C@H]3N(C4=NC(N)=NC=C4C(C)=O)CC3)=NN5C1=C(C=C5)Cl
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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