PIK-93
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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.

Chemical Structure

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PIK-93
CAS# 593960-11-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406325
Name: PIK-93
CAS#: 593960-11-3
Chemical Formula: C14H16ClN3O4S2
Exact Mass: 389.03
Molecular Weight: 389.869
Elemental Analysis: C, 43.13; H, 4.14; Cl, 9.09; N, 10.78; O, 16.41; S, 16.45

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2450 2 Weeks
1g USD 3450 2 Weeks
2g USD 5450 2 Weeks
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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

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Product Data:
Product Data
Instruction:
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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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 5.0 12.82
DMSO 61.0 156.46
Ethanol 0.6 1.60

Preparing Stock Solutions

The following data is based on the product molecular weight 389.87 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. 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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1. Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. By Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. From PCT Int. Appl. (2013), WO 2013147649 A2 20131003,

2. Phosphatidylinositol 4-kinase III beta is essential for replication of human rhinovirus and its inhibition causes a lethal phenotype in vivo. By Spickler, Catherine; Lippens, Julie; Laberge, Marie-Kristine; Desmeules, Sophie; Bellavance, Edith; Garneau, Michel; Guo, Tim; Hucke, Oliver; Leyssen, Pieter; Neyts, Johan; et al. From Antimicrobial Agents and Chemotherapy (2013), 57(7), 3358-3368. ,

3. Autoimmune and inflammatory disorder therapy using inhibitors of phosphatidylinositol-4-kinase IIIβ and screening methods thereof By Herman, Jean; Louat, Thierry; Huang, Qiuya; Vanderhoydonck, Bart; Waer, Mark; Herdewijn, Piet From PCT Int. Appl. (2013), WO 2013034738 A1 20130314,

4. Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. By Jane, Stephen M.; Darido, Charbel. From PCT Int. Appl. (2013), WO 2013029116 A1 20130307,

5. Coxsackievirus mutants that can bypass host factor PI4KIIIβ and the need for high levels of PI4P lipids for replication. By van der Schaar, Hilde M.; van der Linden, Lonneke; Lanke, Kjerstin H. W.; Strating, Jeroen R. P. M.; Puerstinger, Gerhard; de Vries, Erik; de Haan, Cornelis A. M.; Neyts, Johan; van Kuppeveld, Frank J. M. From Cell Research (2012), 22(11), 1576-1592. , DOI:10.1038/cr.2012.129

6. Methods for treating oncovirus positive cancers. By Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. From PCT Int. Appl. (2012), WO 2012118978 A1 20120907,

7. Methods and compositions targeting signaling pathways for the treatment of cancer By Brugge, Joan S.; Muranen, Taru; Mills, Gordon; Selfors, Laura. From PCT Int. Appl. (2011), WO 2011133668 A2 20111027,

8. Phosphatidylinositol 4-kinase III beta is a target of enviroxime-like compounds for antipoliovirus activity By Arita, Minetaro; Kojima, Hirotatsu; Nagano, Tetsuo; Okabe, Takayoshi; Wakita, Takaji; Shimizu, Hiroyuki. From Journal of Virology (2011), 85(5), 2364-2372. , DOI:10.1128/JVI.02249-10

9. Modification of proteins for detection in cellular assays By Treiber, Daniel Kelly; Lewis, Warren G.; Wodicka, Lisa M. From PCT Int. Appl. (2010), WO 2010124157 A1 20101028,

10. Shaping Development of Autophagy Inhibitors with the Structure of the Lipid Kinase Vps34 By Miller, Simon; Tavshanjian, Brandon; Oleksy, Arkadiusz; Perisic, Olga; Houseman, Benjamin T.; Shokat, Kevan M.; Williams, Roger L. From Science (Washington, DC, United States) (2010), 327(5973), 1638-1642. ,

11. Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110α By Zunder, Eli R.; Knight, Zachary A.; Houseman, Benjamin T.; Apsel, Beth; Shokat, Kevan M. From Cancer Cell (2008), 14(2), 180-192. , DOI:10.1016/j.ccr.2008.06.014

12. Phosphoinositide modulation for the treatment of neurodegenerative diseases By Kim, Tae-Wan; Dipaolo, Gilbert; Kang, Min Suk; Berman, Diego; McIntire, Laura Beth Johnson From PCT Int. Appl. (2008), WO 2008064244 A2 20080529,

13. Design of Drug-Resistant Alleles of Type-III Phosphatidylinositol 4-Kinases Using Mutagenesis and Molecular Modeling By Balla, Andras; Tuymetova, Galina; Toth, Balazs; Szentpetery, Zsofia; Zhao, Xiaohang; Knight, Zachary A.; Shokat, Kevan; Steinbach, Peter J.; Balla, Tamas From Biochemistry (2008), 47(6), 1599-1607. , DOI:10.1021/bi7017927

14. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling By Knight, Zachary A.; Gonzalez, Beatriz; Feldman, Morri E.; Zunder, Eli R.; Goldenberg, David D.; Williams, Olusegun; Loewith, Robbie; Stokoe, David; Balla, Andras; Toth, Balazs; et al From Cell (Cambridge, MA, United States) (2006), 125(4), 733-747. ,

15. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma . By Fan, Qi-Wen; Knight, Zachary A.; Goldenberg, David D.; Yu, Wei; Mostov, Keith E.; Stokoe, David; Shokat, Kevan M.; Weiss, William A. From Cancer Cell (2006), 9(5), 341-349.

16. 5-Phenylthiazole derivatives and their use as phosphatidylinositol 3-kinase (Pi3K) inhibitors for the treatment of allergic and inflammatory diseases. By Bruce, Ian; Finan, Peter; Leblanc, Catherine; McCarthy, Clive; Whitehead, Lewis; Blair, Nicola Elaine; Bloomfield, Graham Charles; Hayler, Judy; Kirman, Louise; Oza, Mrinalini Sachin; et al. From PCT Int. Appl. (2003), WO 2003072557 A1 20030904,