LH1306
LH1306 is a C2-symmetric inhibitor of PD-1/PD-L1 protein-protein interaction (PPI), with an IC50 value of 25 nM. LH1306 can be used in anti-tumor research.
For research use only. We do not sell to patients.
- CAS No.: 2182653-84-3
- Formula: C38H48N6O6
- Molecular Weight:684.82
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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
IC50: 25 nM (PD-1/PD-L1)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | GI50 |
3.1 μM
Compound: 2a
|
Cytotoxicity against CHOK1 cells stably expressing human PDL1 co-cultured with human Jurkat T cell expressing human PD1 assessed as growth inhibition measured after 24 hrs by XTT assay
Cytotoxicity against CHOK1 cells stably expressing human PDL1 co-cultured with human Jurkat T cell expressing human PD1 assessed as growth inhibition measured after 24 hrs by XTT assay
|
[PMID: 31298541] |
| HEK293 | IC50 |
25 nM
Compound: 2a
|
Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 1 hr by APC-labeled anti-His antibody/Eu-
Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 1 hr by APC-labeled anti-His antibody/Eu-
|
[PMID: 31298541] |
| Jurkat | EC50 |
334 nM
Compound: 2a
|
Inhibition of PD1/PDL1 interaction in human Jurkat cells co-cultured with human U2OS cells expressing PDL1 assessed as reduction in SHP1 recruitment preincubated with U2OS cells for 60 mins followed by Jurkat cell addition and measured after 2 hrs by Path
Inhibition of PD1/PDL1 interaction in human Jurkat cells co-cultured with human U2OS cells expressing PDL1 assessed as reduction in SHP1 recruitment preincubated with U2OS cells for 60 mins followed by Jurkat cell addition and measured after 2 hrs by Path
|
[PMID: 31298541] |
| Jurkat | EC50 |
4214 nM
Compound: 2a
|
Inhibition of human PD1 stably expressed in human Jurkat T cells co-expressing NFAT-induced luciferase/human PDL1 stably expressed in CHOK1 cells co-expressing aAPC protein-protein interaction assessed as increase in NFAT signaling measured after 6 hrs by
Inhibition of human PD1 stably expressed in human Jurkat T cells co-expressing NFAT-induced luciferase/human PDL1 stably expressed in CHOK1 cells co-expressing aAPC protein-protein interaction assessed as increase in NFAT signaling measured after 6 hrs by
|
[PMID: 31298541] |
| Jurkat | GI50 |
3.1 μM
Compound: 2a
|
Cytotoxicity against human Jurkat T cell expressing human PD1 co-cultured with CHOK1 cells stably expressing human PDL1 assessed as growth inhibition measured after 24 hrs by XTT assay
Cytotoxicity against human Jurkat T cell expressing human PD1 co-cultured with CHOK1 cells stably expressing human PDL1 assessed as growth inhibition measured after 24 hrs by XTT assay
|
[PMID: 31298541] |
Chemical Information
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CAS No. 2182653-84-3
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Molecular Weight 684.82
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Formula C38H48N6O6
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SMILES
CC(NCCNCC(C(OC)=N1)=CC=C1OCC2=CC=CC(C3=CC=CC(COC4=CC=C(C(OC)=N4)CNCCNC(C)=O)=C3C)=C2C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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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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