1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. 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.

LH1306 Chemical Structure

LH1306 Chemical Structure

CAS No. : 2182653-84-3

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Description

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[1].

IC50 & Target

IC50: 25 nM (PD-1/PD-L1)[1].

Cellular Effect
Cell Line 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 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]
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]
Molecular Weight

684.82

Formula

C38H48N6O6

CAS No.
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

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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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.

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LH1306
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HY-132223
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