LH1307
Based on 1 Customer Validation
LH1307 is a C2-symmetric inhibitor of PD-1/PD-L1 protein-protein interactions with a IC50 value of 3.0 μM and can be used in cancer studies.
For research use only. We do not sell to patients.
- Purity: 96.9%
- CAS No.: 2375720-38-8
- Formula: C54H58N8O6
- Molecular Weight:915.09
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 3.0 μM (PD-1/PD-L1)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | GI50 |
11.8 μM
Compound: 2b
|
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 |
3 nM
Compound: 2b
|
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 |
763 nM
Compound: 2b
|
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 | EC50 |
79 nM
Compound: 2b
|
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 | GI50 |
11.8 μM
Compound: 2b
|
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. 2375720-38-8
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Appearance Solid
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Molecular Weight 915.09
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Formula C54H58N8O6
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Color Off-white to light yellow
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SMILES
N#CC1=CN=CC(COC2=CC(OCC3=CC=CC(C4=CC=CC(COC5=C(C)C=C(CNCCNC(C)=O)C(OCC6=CC(C#N)=CN=C6)=C5)=C4C)=C3C)=C(C)C=C2CNCCNC(C)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (264 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)