ZLDI-8
new
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 462439

CAS#: 667880-38-8

Description: ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor.


Chemical Structure

img
ZLDI-8
CAS# 667880-38-8

Theoretical Analysis

MedKoo Cat#: 462439
Name: ZLDI-8
CAS#: 667880-38-8
Chemical Formula: C24H23N3O3S
Exact Mass: 433.15
Molecular Weight: 433.526
Elemental Analysis: C, 66.49; H, 5.35; N, 9.69; O, 11.07; S, 7.40

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 450 Ready to ship
50mg USD 750 Ready to ship
100mg USD 1250 Ready to ship
200mg USD 2050 Ready to ship
500mg USD 3650 Ready to ship
Bulk inquiry

Synonym: ZLDI-8; ZLDI-8; ZLDI-8

IUPAC/Chemical Name: 5-((1-(2-(2,4-dimethylphenoxy)ethyl)-2-methyl-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

InChi Key: GNBZGGYWSRGVBG-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23N3O3S/c1-14-8-9-21(15(2)12-14)30-11-10-27-16(3)18(17-6-4-5-7-20(17)27)13-19-22(28)25-24(31)26-23(19)29/h4-9,12-13H,10-11H2,1-3H3,(H2,25,26,28,29,31)

SMILES Code: O=C(/C(C(N1)=O)=C/C2=C(C)N(CCOC3=CC=C(C)C=C3C)C4=C2C=CC=C4)NC1=S

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
In vitro activity: ZLDI-8 is a potential candidate for improving colorectal cancer (CRC) treatment outcomes. ZLDI-8 demonstrated specific inhibition of CRC cell proliferation by targeting ADAM17 and the Notch pathway. ZLDI-8 showed promising potential as a chemosensitizer, enhancing the anti-tumor and anti-metastasis effects of chemotherapy drugs, such as 5-fluorouracil and irinotecan, by reversing Notch and epithelial-mesenchymal transition (EMT) pathways. Reference: Cell Prolif. 2018 Oct;51(5):e12480. https://pubmed.ncbi.nlm.nih.gov/30069943/
In vivo activity: ZLDI-8 has potential as an effective agent in the treatment of drug-resistant lung cancer. ZLDI-8 suppressed multidrug-resistant lung cancer xenograft growth and blocks metastasis in a tail vein injection mice model. Reference: Pharmacol Res. 2019 Oct;148:104406. https://pubmed.ncbi.nlm.nih.gov/31442576/

Preparing Stock Solutions

The following data is based on the product molecular weight 433.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lu H, Wu C, Jiang XW, Zhao Q. ZLDI-8 suppresses angiogenesis and vasculogenic mimicry in drug-resistant NSCLC in vitro and in vivo. Lung Cancer. 2023 Aug;182:107279. doi: 10.1016/j.lungcan.2023.107279. Epub 2023 Jun 14. PMID: 37364397. 2. Li DD, Zhao CH, Ding HW, Wu Q, Ren TS, Wang J, Chen CQ, Zhao QC. A novel inhibitor of ADAM17 sensitizes colorectal cancer cells to 5-Fluorouracil by reversing Notch and epithelial-mesenchymal transition in vitro and in vivo. Cell Prolif. 2018 Oct;51(5):e12480. doi: 10.1111/cpr.12480. Epub 2018 Aug 2. PMID: 30069943; PMCID: PMC6528951. 3. Lu HY, Chu HX, Tan YX, Qin XC, Liu MY, Li JD, Ren TS, Zhang YS, Zhao QC. Novel ADAM-17 inhibitor ZLDI-8 inhibits the metastasis of hepatocellular carcinoma by reversing epithelial-mesenchymal transition in vitro and in vivo. Life Sci. 2020 Mar 1;244:117343. doi: 10.1016/j.lfs.2020.117343. Epub 2020 Jan 21. PMID: 31978449. 4. Lu HY, Zu YX, Jiang XW, Sun XT, Liu TY, Li RL, Wu Q, Zhang YS, Zhao QC. Novel ADAM-17 inhibitor ZLDI-8 inhibits the proliferation and metastasis of chemo-resistant non-small-cell lung cancer by reversing Notch and epithelial mesenchymal transition in vitro and in vivo. Pharmacol Res. 2019 Oct;148:104406. doi: 10.1016/j.phrs.2019.104406. Epub 2019 Aug 20. PMID: 31442576.
In vitro protocol: 1. Lu H, Wu C, Jiang XW, Zhao Q. ZLDI-8 suppresses angiogenesis and vasculogenic mimicry in drug-resistant NSCLC in vitro and in vivo. Lung Cancer. 2023 Aug;182:107279. doi: 10.1016/j.lungcan.2023.107279. Epub 2023 Jun 14. PMID: 37364397. 2. Li DD, Zhao CH, Ding HW, Wu Q, Ren TS, Wang J, Chen CQ, Zhao QC. A novel inhibitor of ADAM17 sensitizes colorectal cancer cells to 5-Fluorouracil by reversing Notch and epithelial-mesenchymal transition in vitro and in vivo. Cell Prolif. 2018 Oct;51(5):e12480. doi: 10.1111/cpr.12480. Epub 2018 Aug 2. PMID: 30069943; PMCID: PMC6528951.
In vivo protocol: 1. Lu HY, Chu HX, Tan YX, Qin XC, Liu MY, Li JD, Ren TS, Zhang YS, Zhao QC. Novel ADAM-17 inhibitor ZLDI-8 inhibits the metastasis of hepatocellular carcinoma by reversing epithelial-mesenchymal transition in vitro and in vivo. Life Sci. 2020 Mar 1;244:117343. doi: 10.1016/j.lfs.2020.117343. Epub 2020 Jan 21. PMID: 31978449. 2. Lu HY, Zu YX, Jiang XW, Sun XT, Liu TY, Li RL, Wu Q, Zhang YS, Zhao QC. Novel ADAM-17 inhibitor ZLDI-8 inhibits the proliferation and metastasis of chemo-resistant non-small-cell lung cancer by reversing Notch and epithelial mesenchymal transition in vitro and in vivo. Pharmacol Res. 2019 Oct;148:104406. doi: 10.1016/j.phrs.2019.104406. Epub 2019 Aug 20. PMID: 31442576.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Zhang Y, Li D, Jiang Q, et al. Novel ADAM-17 inhibitor ZLDI-8 enhances the in vitro and in vivo chemotherapeutic effects of Sorafenib on hepatocellular carcinoma cells. Cell Death Dis. 2018;9(7):743. Published 2018 Jul 3. doi:10.1038/s41419-018-0804-6

2: Hou X, Li R, Li K, Yu X, Sun JP, Fang H. Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening. J Med Chem. 2014;57(22):9309-9322. doi:10.1021/jm500692u.