2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. PD-1/PD-L1-IN-29

PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity.

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PD-1/PD-L1-IN-29 Chemical Structure

PD-1/PD-L1-IN-29 Chemical Structure

CAS No. : 2665734-13-2

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5 mg USD 850 In-stock
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Based on 1 publication(s) in Google Scholar

PD-1/PD-L1-IN-29 Related Antibodies

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Description

PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity[1].

In Vitro

PD-1/PD-L1-IN-29(S4-1) (10 or 20 μM, 48 h) can increase the cytotoxicity of PBMCs against A375 tumor cells by blocking PD-1/PD-L1 interaction and restoring the activation state of PBMCs, with little direct killing effect on tumor cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PD-1/PD-L1-IN-29 Related Antibodies
In Vivo

PD-1/PD-L1-IN-29(S4-1)(10 or 25 mg/kg, i.p., 12 days) significantly inhibits tumour growth in the MC38 colorectal tumour mouse model, as observed in both the low and high dose groups (10 and 25 mg/kg), with inhibition rates of 65.9% and 88.8% respectively[1].
The pharmacokinetic parameters of PD-1/PD-L1-IN-29(S4-1) in mice

Parameters iv (5 mg/kg) po (50 mg/kg)
T1/2 (h) 9.78 4.77
Tmax (h) 0.08 0.92
Cmax (ng/mL) 6290 260.67
AUC0-t (h*ng/mL) 3466.58/td> 808.04
AUC0-∞ (h*ng/mL) 3566.62 830.34
CL (mL/h/kg) 1404.22 -

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

460.48

Formula

C26H24N2O6
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

OC[C@H](NCC1=CC2=C(C=C1OC)C(N(C2=O)C3=C(C(C4=CC=CC=C4)=CC=C3)C)=O)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (144.78 mM; ultrasonic and adjust pH to 2 with 1M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1716 mL 10.8582 mL 21.7165 mL
5 mM 0.4343 mL 2.1716 mL 4.3433 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1716 mL 10.8582 mL 21.7165 mL 54.2912 mL
5 mM 0.4343 mL 2.1716 mL 4.3433 mL 10.8582 mL
10 mM 0.2172 mL 1.0858 mL 2.1716 mL 5.4291 mL
15 mM 0.1448 mL 0.7239 mL 1.4478 mL 3.6194 mL
20 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7146 mL
25 mM 0.0869 mL 0.4343 mL 0.8687 mL 2.1716 mL
30 mM 0.0724 mL 0.3619 mL 0.7239 mL 1.8097 mL
40 mM 0.0543 mL 0.2715 mL 0.5429 mL 1.3573 mL
50 mM 0.0434 mL 0.2172 mL 0.4343 mL 1.0858 mL
60 mM 0.0362 mL 0.1810 mL 0.3619 mL 0.9049 mL
80 mM 0.0271 mL 0.1357 mL 0.2715 mL 0.6786 mL
100 mM 0.0217 mL 0.1086 mL 0.2172 mL 0.5429 mL
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PD-1/PD-L1-IN-29 Related Classifications

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.

Keywords:

PD-1/PD-L1-IN-292665734-13-2PD-1/PD-L1PD-1/Programmed death-ligand 1endoplasmic reticulumanticancerInhibitorinhibitorinhibit

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