Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
PFI-2 HCl, the hydrochloride salt of PFI-2, is a selective, and cell-active lysine methyltransferase SETD7 inhibitor with potential antitumor activity. It inhibits SETD7 with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. In HEK293 cells, (R)-PFI-2 (10 µM) bound to and stabilized SETD7. In Setd7+/+ murine embryonic fibroblasts (MEFs), (R)-PFI-2 increased nuclear localization of Yes-associated protein (YAP) and the expression of YAP target genes Ctgf, Gli2 and Cdc20.
ln Vitro |
(R)-PFI-2 hydrochloride inhibits with a high IC50 of 2.0 nM, while (S)-PFI-2 hydrochloride has an IC50 of 1.0 μM [1].
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ln Vivo |
PFI-2 hydrochloride (ip, 200 μM, twice weekly) reduces the progression of renal fibrosis and protects renal function in FA nephropathy [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) decreases ECM buildup and fibroblast activation following FA damage [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) suppresses Th2 cytokine signaling activation and M2 macrophage polarization [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) reduces M2 macrophage-myofibroblast transition and bone marrow myofibroblast accumulation in FA-treated kidneys [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) attenuates macrophage M2 polarization and M2 macrophage to myofibroblast transition in obstructed kidneys [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) reduces myeloid myofibroblast aggregation and renal fibrosis after UUO damage [2]. PFI-2 hydrochloride (ip, 200 μM, twice weekly) decreases inflammatory cell infiltration, inflammatory chemical synthesis, and NF-κB activation in FA nephropathy [2].
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Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8-10-week old, 20-25 g)[2]
Doses: 200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL) Route of Administration: intraperitoneal (ip)injection, twice a week Experimental Results: Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01). decreased the infiltration of inflammatory cells and diminished the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01). Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01). |
References |
[1]. Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547.
[2]. Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097. |
Molecular Formula |
C23H25F4N3O3S.HCL
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Molecular Weight |
535.98
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CAS # |
1627607-87-7
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Related CAS # |
PFI-2;1627676-59-8
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SMILES |
Cl.S(C1C=C(C2CNCCC=2C=1)F)(N[C@H](CC1C=CC=C(C(F)(F)F)C=1)C(N1CCCC1)=O)(=O)=O
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InChi Key |
ZADKZNVAJGEFLC-ZMBIFBSDSA-N
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InChi Code |
InChI=1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27;/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2;1H/t21-;/m1./s1
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Chemical Name |
(R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1 mg/mL (1.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8657 mL | 9.3287 mL | 18.6574 mL | |
5 mM | 0.3731 mL | 1.8657 mL | 3.7315 mL | |
10 mM | 0.1866 mL | 0.9329 mL | 1.8657 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.