PAFAH1b2 | CAS#942285-55-4 | 1b2 and 1b3 inhibitor

MedKoo Cat#: 562552 | Name: PAFAH1b2

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Description:

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

PAFAH1b2 is a selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3. It acts by impairing cancer cell survival. PAFAH1b2 is one of the multiple enzymes found in PAF degradation.

Chemical Structure

PAFAH1b2

CAS#942285-55-4

Theoretical Analysis

MedKoo Cat#: 562552

Name: PAFAH1b2

CAS#: 942285-55-4

Chemical Formula: C30H33NO4S

Exact Mass: 503.2130

Molecular Weight: 503.66

Elemental Analysis: C, 71.54; H, 6.60; N, 2.78; O, 12.71; S, 6.37

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 400.00
5mg	USD 600.00
10mg	USD 1,000.00

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Synonym

PAFAH1b2; PAFAH-1-b-2; PAFAH 1 b 2; 3-IN-P11; 3 IN P11; 3INP11; 3 inhibitor P11; 3-inhibitor-P11; P11; P-11; P 11;

IUPAC/Chemical Name

(2R,6R)-rel-2-[4-(1,1-dimethylethyl)phenyl]-1,2,5,6-tetrahydro-6-(4-methylphenyl)-1-[(4-methylphenyl)sulfonyl]-3-pyridinecarboxylic acid

InChi Key

KUBDPRSHRVANQQ-VSGBNLITSA-N

InChi Code

InChI=1S/C30H33NO4S/c1-20-6-10-22(11-7-20)27-19-18-26(29(32)33)28(23-12-14-24(15-13-23)30(3,4)5)31(27)36(34,35)25-16-8-21(2)9-17-25/h6-18,27-28H,19H2,1-5H3,(H,32,33)/t27-,28-/m1/s1

SMILES Code

O=C(C1=CC[C@H](C2=CC=C(C)C=C2)N(S(=O)(C3=CC=C(C)C=C3)=O)[C@@H]1C4=CC=C(C(C)(C)C)C=C4)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

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

>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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PAFAH1b2 is a selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3.

In vitro activity:

Here, this study reports a class of tetrahydropyridine reversible inhibitors of PAFAH1b2/3 discovered using a fluorescence polarization-activity-based protein profiling (fluopol-ABPP) screen of the NIH 300,000+ compound library. The most potent of these agents, P11, exhibited IC50 values of ∼40 and 900 nM for PAFAH1b2 and 1b3, respectively. This study confirms selective inhibition of PAFAH1b2/3 in cancer cells by P11 using an ABPP protocol adapted for in situ analysis of reversible inhibitors and show that this compound impairs tumor cell survival, supporting a role for PAFAH1b2/3 in cancer. Reference: ACS Chem Biol. 2015 Apr 17;10(4):925-32. https://pubmed.ncbi.nlm.nih.gov/25602368/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO:PBS (pH 7.2) (1:1)	0.5	0.99

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 503.66 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:

Chang JW, Zuhl AM, Speers AE, Niessen S, Brown SJ, Mulvihill MM, Fan YC, Spicer TP, Southern M, Scampavia L, Fernandez-Vega V, Dix MM, Cameron MD, Hodder PS, Rosen H, Nomura DK, Kwon O, Hsu KL, Cravatt BF. Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival. ACS Chem Biol. 2015 Apr 17;10(4):925-32. doi: 10.1021/cb500893q. Epub 2015 Jan 20. PMID: 25602368; PMCID: PMC4402257.

In vitro protocol:

In vivo protocol:

TBD

1: Ishino T, Oda T, Kawasumi T, Takemoto K, Nishida M, Horibe Y, Chikuie N, Taruya T, Hamamoto T, Ueda T, Takeno S. Severe Type 2 Inflammation Leads to High Platelet-Activating-Factor-Associated Pathology in Chronic Rhinosinusitis with Nasal Polyps-A Hierarchical Cluster Analysis Using Bulk RNA Barcoding and Sequencing. Int J Mol Sci. 2024 Feb 9;25(4):2113. doi: 10.3390/ijms25042113. PMID: 38396790; PMCID: PMC10889510. 2: Ho CY, Lee JI, Huang SP, Chen SC, Geng JH. A Genome-Wide Association Study of Metabolic Syndrome in the Taiwanese Population. Nutrients. 2023 Dec 25;16(1):77. doi: 10.3390/nu16010077. PMID: 38201907; PMCID: PMC10780952. 3: Li L, Xin Q, Zhang L, Miao Z, Zhu Z, Huang Q, Zheng N. Analysis of circRNA- miRNA-mRNA regulatory network of embryonic gonadal development in Mulard duck. Poult Sci. 2024 Feb;103(2):103303. doi: 10.1016/j.psj.2023.103303. Epub 2023 Nov 25. PMID: 38096667; PMCID: PMC10762475. 4: Zeng W, Xie F, Pan Y, Chen Z, Chen H, Liu X, Tian K, Xu D. A comprehensive prognostic score for head and neck squamous cancer driver genes and phenotype traits. Discov Oncol. 2023 Oct 28;14(1):193. doi: 10.1007/s12672-023-00796-y. PMID: 37897503; PMCID: PMC10613197. 5: Wang Q, Shi Q, Wang Z, Lu J, Hou J. Integrating plasma proteomes with genome- wide association data for causal protein identification in multiple myeloma. BMC Med. 2023 Sep 29;21(1):377. doi: 10.1186/s12916-023-03086-0. PMID: 37775746; PMCID: PMC10542236. 6: Sui L, Sanders A, Jiang WG, Ye L. Deregulated molecules and pathways in the predisposition and dissemination of breast cancer cells to bone. Comput Struct Biotechnol J. 2022 May 30;20:2745-2758. doi: 10.1016/j.csbj.2022.05.051. PMID: 35685372; PMCID: PMC9168524. 7: Tanigawa K, Kiriya M, Hayashi Y, Shinden Y, Kijima Y, Natsugoe S, Sumimoto T, Morimoto-Kamata R, Yui S, Hama K, Yokoyama K, Nakamura Y, Suzuki K, Nojiri H, Inoue K, Karasawa K. Cathepsin G-induced malignant progression of MCF-7 cells involves suppression of PAF signaling through induced expression of PAFAH1B2. Biochim Biophys Acta Mol Cell Biol Lipids. 2022 Aug;1867(8):159164. doi: 10.1016/j.bbalip.2022.159164. Epub 2022 Apr 22. PMID: 35462067. 8: Zhang Q, Lv L, Ma P, Zhang Y, Deng J, Zhang Y. Identification of an Autophagy-Related Pair Signature for Predicting Prognoses and Immune Activity in Pancreatic Adenocarcinoma. Front Immunol. 2021 Dec 9;12:743938. doi: 10.3389/fimmu.2021.743938. PMID: 34956177; PMCID: PMC8695429. 9: Kim GR, Zhao T, Kee HJ, Kee SJ, Jeong MH. MicroRNA-212-5p and its target PAFAH1B2 suppress vascular proliferation and contraction via the downregulation of RhoA. PLoS One. 2021 Mar 24;16(3):e0249146. doi: 10.1371/journal.pone.0249146. PMID: 33760887; PMCID: PMC7990166. 10: Chen C, Pan Y, Bai L, Chen H, Duan Z, Si Q, Zhu R, Chuang TH, Luo Y. MicroRNA-3613-3p functions as a tumor suppressor and represents a novel therapeutic target in breast cancer. Breast Cancer Res. 2021 Jan 25;23(1):12. doi: 10.1186/s13058-021-01389-9. PMID: 33494814; PMCID: PMC7836180. 11: Xu ZY, Peng J, Shi ZZ, Chen XL, Cheng HZ, Wang H, Wang Y, Wang GP, Jiang W, Peng H. Silencing linc00662 inhibits cell proliferation and colony formation of lung cancer cells via regulating the miR-145-5p-PAFAH1B2 axis. Biochem Cell Biol. 2021 Jun;99(3):330-338. doi: 10.1139/bcb-2019-0396. Epub 2020 Oct 27. PMID: 33108738. 12: Gardner OK, Wang L, Van Booven D, Whitehead PL, Hamilton-Nelson KL, Adams LD, Starks TD, Hofmann NK, Vance JM, Cuccaro ML, Martin ER, Byrd GS, Haines JL, Bush WS, Beecham GW, Pericak-Vance MA, Griswold AJ. RNA editing alterations in a multi-ethnic Alzheimer disease cohort converge on immune and endocytic molecular pathways. Hum Mol Genet. 2019 Sep 15;28(18):3053-3061. doi: 10.1093/hmg/ddz110. PMID: 31162550; PMCID: PMC6737295. 13: Carratala-Marco F, Andreo-Lillo P, Martinez-Morga M, Escamez-Martínez T, Botella-López A, Bueno C, Martinez S. Clinical Phenotypes Associated to Engrailed 2 Gene Alterations in a Series of Neuropediatric Patients. Front Neuroanat. 2018 Aug 10;12:61. doi: 10.3389/fnana.2018.00061. PMID: 30147646; PMCID: PMC6095973. 14: Ma C, Guo Y, Zhang Y, Duo A, Jia Y, Liu C, Li B. PAFAH1B2 is a HIF1a target gene and promotes metastasis in pancreatic cancer. Biochem Biophys Res Commun. 2018 Jun 27;501(3):654-660. doi: 10.1016/j.bbrc.2018.05.039. Epub 2018 May 16. PMID: 29758199. 15: Ding X, Yu R, Wang X, Wu W, Peng B, Liu H, Geng Y, Dong F, Lu J, Yu M, Fang S. [Proteome Profiling of A549 Cells Infected with Influenza H7N9 Virus]. Bing Du Xue Bao. 2016 Sep;32(5):574-81. Chinese. PMID: 30001579. 16: Ding X, Lu J, Yu R, Wang X, Wang T, Dong F, Peng B, Wu W, Liu H, Geng Y, Zhang R, Ma H, Cheng J, Yu M, Fang S. Preliminary Proteomic Analysis of A549 Cells Infected with Avian Influenza Virus H7N9 and Influenza A Virus H1N1. PLoS One. 2016 May 25;11(5):e0156017. doi: 10.1371/journal.pone.0156017. PMID: 27223893; PMCID: PMC4880285. 17: Sarma BK, Liu X, Kodadek T. Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library. Bioorg Med Chem. 2016 Sep 1;24(17):3953-3963. doi: 10.1016/j.bmc.2016.04.047. Epub 2016 Apr 23. PMID: 27160052; PMCID: PMC4972644. 18: Gombojav B, Lee SJ, Kho M, Song YM, Lee K, Sung J. Multiple susceptibility loci at chromosome 11q23.3 are associated with plasma triglyceride in East Asians. J Lipid Res. 2016 Feb;57(2):318-24. doi: 10.1194/jlr.P063461. Epub 2015 Dec 3. PMID: 26634697; PMCID: PMC4727427. 19: Kohnz RA, Mulvihill MM, Chang JW, Hsu KL, Sorrentino A, Cravatt BF, Bandyopadhyay S, Goga A, Nomura DK. Activity-Based Protein Profiling of Oncogene-Driven Changes in Metabolism Reveals Broad Dysregulation of PAFAH1B2 and 1B3 in Cancer. ACS Chem Biol. 2015 Jul 17;10(7):1624-30. doi: 10.1021/acschembio.5b00053. Epub 2015 May 7. PMID: 25945974; PMCID: PMC4702252. 20: Ferreiro JF, Morscio J, Dierickx D, Marcelis L, Verhoef G, Vandenberghe P, Tousseyn T, Wlodarska I. Post-transplant molecularly defined Burkitt lymphomas are frequently MYC-negative and characterized by the 11q-gain/loss pattern. Haematologica. 2015 Jul;100(7):e275-9. doi: 10.3324/haematol.2015.124305. Epub 2015 Mar 20. PMID: 25795716; PMCID: PMC4486241.