WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406325
CAS#: 593960-11-3
Description: PIK-93 is a potent PI3K inhibitor. PIK93 selectively inhibits the type III PI 4-kinase beta enzyme, and small interfering RNA-mediated down-regulation of the individual PI 4-kinase enzymes, revealed that PI 4-kinase beta has a dominant role in ceramide transport between the ER and Golgi.
MedKoo Cat#: 406325
Name: PIK-93
CAS#: 593960-11-3
Chemical Formula: C14H16ClN3O4S2
Exact Mass: 389.0271
Molecular Weight: 389.869
Elemental Analysis: C, 43.13; H, 4.14; Cl, 9.09; N, 10.78; O, 16.41; S, 16.45
Related CAS #: 593960-11-3
Synonym: PIK93; PIK 93; PIK-93.
IUPAC/Chemical Name: N-(5-(4-chloro-3-(N-(2-hydroxyethyl)sulfamoyl)phenyl)-4-methylthiazol-2-yl)acetamide
InChi Key: JFVNFXCESCXMBC-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H16ClN3O4S2/c1-8-13(23-14(17-8)18-9(2)20)10-3-4-11(15)12(7-10)24(21,22)16-5-6-19/h3-4,7,16,19H,5-6H2,1-2H3,(H,17,18,20)
SMILES Code: CC(NC1=NC(C)=C(C2=CC=C(Cl)C(S(=O)(NCCO)=O)=C2)S1)=O
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: 0– 4 oC for short term (weeks to 1 month) or -20 oC for long terms (months to years).
Solubility: soluble in DMSO
Shelf Life: >2 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
| Biological target: | PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM. |
| In vitro activity: | This study aimed to discover small-molecule drugs that can modulate the TME to enhance ICI treatment efficacy in NSCLC in vitro and in vivo. This study identified a PD-L1 protein-modulating small molecule, PIK-93, using a cell-based global protein stability (GPS) screening system. PIK-93 mediated PD-L1 ubiquitination by enhancing the PD-L1-Cullin-4A interaction. PIK-93 reduced PD-L1 levels on M1 macrophages and enhanced M1 antitumor cytotoxicity. Reference: Sci Adv. 2023 Apr 7;9(14):eade9944. https://pubmed.ncbi.nlm.nih.gov/37027467/ |
| In vivo activity: | When given to vpr-1 knockdown worms, PIK-93 significantly reduced the frequency of worms with DA neuronal loss from Day 6 to 10 (Fig. 7b). Worms treated with PIK-93 exhibited significantly lower instances of DA neuronal loss at Day 6 and Day 10 (15.0% ± 2.2% and 33.7% ± 2.9%, respectively, p < 0.001) when compared to mock treated control (27.3% ± 2.7% and 44.9% ± 3.2% at Day 6 and Day 10, respectively, p < 0.001). The inhibitor had no effect on DB neuron survival. Together, this indicates that inhibiting PtdIns 4-kinase activity reduced the frequency of DA neuronal loss caused by the knockdown of vpr-1 in these neurons. Reference: Sci Rep. 2017 Sep 14;7(1):11582. https://pubmed.ncbi.nlm.nih.gov/28912432/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 5.0 | 12.82 | |
| DMSO | 61.0 | 156.46 | |
| Ethanol | 0.63 | 1.6 |
The following data is based on the product molecular weight 389.869 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.
| 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. Lin CY, Huang KY, Kao SH, Lin MS, Lin CC, Yang SC, Chung WC, Chang YH, Chein RJ, Yang PC. Small-molecule PIK-93 modulates the tumor microenvironment to improve immune checkpoint blockade response. Sci Adv. 2023 Apr 7;9(14):eade9944. doi: 10.1126/sciadv.ade9944. Epub 2023 Apr 7. PMID: 37027467; PMCID: PMC10081850. 2. Hanes CM, D'Amico AE, Ueyama T, Wong AC, Zhang X, Hynes WF, Barroso MM, Cady NC, Trebak M, Saito N, Lennartz MR. Golgi-Associated Protein Kinase C-ε Is Delivered to Phagocytic Cups: Role of Phosphatidylinositol 4-Phosphate. J Immunol. 2017 Jul 1;199(1):271-277. doi: 10.4049/jimmunol.1700243. Epub 2017 May 24. PMID: 28539432; PMCID: PMC5505341. |
| In vitro protocol: | 1. Lin CY, Huang KY, Kao SH, Lin MS, Lin CC, Yang SC, Chung WC, Chang YH, Chein RJ, Yang PC. Small-molecule PIK-93 modulates the tumor microenvironment to improve immune checkpoint blockade response. Sci Adv. 2023 Apr 7;9(14):eade9944. doi: 10.1126/sciadv.ade9944. Epub 2023 Apr 7. PMID: 37027467; PMCID: PMC10081850. 2. Hanes CM, D'Amico AE, Ueyama T, Wong AC, Zhang X, Hynes WF, Barroso MM, Cady NC, Trebak M, Saito N, Lennartz MR. Golgi-Associated Protein Kinase C-ε Is Delivered to Phagocytic Cups: Role of Phosphatidylinositol 4-Phosphate. J Immunol. 2017 Jul 1;199(1):271-277. doi: 10.4049/jimmunol.1700243. Epub 2017 May 24. PMID: 28539432; PMCID: PMC5505341. 3. Zhang W, Colavita A, Ngsee JK. Mitigating Motor Neuronal Loss in C. elegans Model of ALS8. Sci Rep. 2017 Sep 14;7(1):11582. doi: 10.1038/s41598-017-11798-6. PMID: 28912432; PMCID: PMC5599522. |
| In vivo protocol: | 1. Zhang W, Colavita A, Ngsee JK. Mitigating Motor Neuronal Loss in C. elegans Model of ALS8. Sci Rep. 2017 Sep 14;7(1):11582. doi: 10.1038/s41598-017-11798-6. PMID: 28912432; PMCID: PMC5599522. |
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