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
Description
IC50 & Target
IC50: 3.0 μM (PD-1/PD-L1)[1].
Cellular Effect
|
Cell Line
|
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
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)