IWP-2
Based on 35 publication(s) in Google Scholar
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 686770-61-6
- Fòrmula: C22H18N4O2S3
- Peso molecular:466.60
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) IWP-2
More- Adv Mater. 2021 Dec;33(49):e2104829. [Abstract]
- Nat Metab. 2026 Jan;8(1):74-95. [Abstract]
- Adv Healthc Mater. 2026 Jun 11:e04956. [Abstract]
- Dev Cell. 2020 Dec 21;55(6):679-694.e11. [Abstract]
- Neoplasia. 2024 Dec 30:60:101096. [Abstract]
- Clin Sci. 2023 Jan 13;137(1):109-127. [Abstract]
- Stem Cell Res Ther. 2024 Oct 8;15(1):350. [Abstract]
- Mol Metab. 2026 Jun:108:102373. [Abstract]
- J Agric Food Chem. 2026 Jun 10;74(22):17392-17404. [Abstract]
- Curr Res Microb Sci. 2026 Jan 27:10:100559. [Abstract]
- Biochem Pharmacol. 2019 Nov;169:113608. [Abstract]
- Stem Cells Transl Med. 2021 May;10(5):743-755. [Abstract]
- Cell Rep Methods. 2024 May 8:100777. [Abstract]
- iScience. 2025 Dec 5;29(1):114355. [Abstract]
- J Inflamm Res. 2024 Nov 19:17:8945-8964. [Abstract]
- J Cell Physiol. 2020 Jul;235(7-8):5811-5822. [Abstract]
- J Gerontol A Biol Sci Med Sci. 2026 Jun 2:glag145. [Abstract]
- Bioengineering (Basel). 2023 Jun 9;10(6):702. [Abstract]
- Microb Pathog. 2024 Sep 21:106960. [Abstract]
- Exp Cell Res. 2022 Nov 11;422(1):113416. [Abstract]
- Autoimmunity. 2023 Dec;56(1):2182741. [Abstract]
- J Appl Polym Sci. 2024 Sep 25.
- eNeuro. 2025 Jan 9:ENEURO.0347-24.2024. [Abstract]
- PLoS One. 2024 Jan 5;19(1):e0287206. [Abstract]
- Toxicon. 2026 Jan:269:108660. [Abstract]
- Exp Ther Med. 2020 Mar;19(3):1701-1710. [Abstract]
- Biocell. 2025 Feb 28.
- Cell Press Blue. 2026 Apr 22.
- Animal Research and One Health. 2026 Mar 19.
- bioRxiv. 2026 Mar 15.
- bioRxiv. 2026 Jan 12.
- bioRxiv. 2024 Mar 13.
- SSRN. 2024 Mar 26.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
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WB
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Flow Cytometry
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RT-PCR
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2D/3D Cell Culture and Differentiation
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RT-PCR
Actividad biológica
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CK1γ2 40 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CAPAN-1 | EC50 |
2.05 μM
Compound: IWP-2
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Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| HEK293 | EC50 |
2.76 μM
Compound: IWP-2
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Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| HT-29 | EC50 |
4.67 μM
Compound: IWP-2
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Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| MIA PaCa-2 | EC50 |
1.9 μM
Compound: IWP-2
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Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| PANC-1 | EC50 |
2.33 μM
Compound: IWP-2
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Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| SW-620 | EC50 |
1.9 μM
Compound: IWP-2
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Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
IWP-2 inhibits the proliferation of the investigated cell lines within the single digit μM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC50s of 8.96 μM, 1.90 μM, 2.33 μM, 3.86 μM, 4.67 μM, 2.76 μM, 1.90 μM and 2.05 μM, respectively[2].
Panc-1 cells are either untreated or treated with 2.33 μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 686770-61-6
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Appearance Solid
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Peso molecular 466.60
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Fòrmula C22H18N4O2S3
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Color White to off-white
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SMILES
O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (35)
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Journal Impact Factor
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Most Recent
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Adv Mater
2021 Dec;33(49):e2104829. PMID: 34632631
IWP-2 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2104829. [Abstract]
ITGA2, ALP and OPN expression in rBMSCs cultured on CBM-CS scaffolds with microbially catalyzed micro/nanostructures for 3 days after blocking Wnt processing by IWP-2 (6 μM; 3 days).
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Nat Metab
2026 Jan;8(1):74-95. PMID: 41507665 -
Adv Healthc Mater
Flexible Sensing Technology for Myocardial Tissue Contractile Force With Integrated Magnetically Actuated Mechanical Stimulation. [Abstract]2026 Jun 11:e04956. PMID: 42277624 -
Dev Cell
Mechanical Tension Promotes Formation of Gastrulation-like Nodes and Patterns Mesoderm Specification in Human Embryonic Stem Cells. [Abstract]2020 Dec 21;55(6):679-694.e11. PMID: 33207224
IWP-2 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2020 Dec 21;55(6):679-694.e11. [Abstract]
Relative mesoderm gene expression levels after 36 h BMP4 plus vehicle (DMSO) or Wnt inhibitor (IWP-2; 2 μM).
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Neoplasia
β-Catenin mediated TAM phenotype promotes pancreatic cancer metastasis via the OSM/STAT3/LOXL2 axis. [Abstract]2024 Dec 30:60:101096. PMID: 39740539
IWP-2 purchased from MedChemExpress. Usage Cited in: Neoplasia. 2024 Dec 30:60:101096. [Abstract]
Western blot analysis of TAM markers following treatment with TCM derived from IWP-2-pretreated (2.5 μM; 6 h) PANC-1 cells (n=3).
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Clin Sci
Chronic GPER activation prompted the proliferation of ileal stem cell in ovariectomized mice depending on Paneth cell-derived Wnt3. [Abstract]2023 Jan 13;137(1):109-127. PMID: 36503938 -
Stem Cell Res Ther
SMYD1 modulates the proliferation of multipotent cardiac progenitor cells derived from human pluripotent stem cells during myocardial differentiation through GSK3β/β-catenin&ERK signaling. [Abstract]2024 Oct 8;15(1):350. PMID: 39380045
IWP-2 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2024 Oct 8;15(1):350. [Abstract]
Flow cytometry for comparisons of TNNT2+ after CHIR-99021 (5 μM; 24 h) and IWP2 (5 μM; 24 h) were added to cells, respectively.
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Mol Metab
2026 Jun:108:102373. PMID: 42025695 -
J Agric Food Chem
T-2 Toxin Induces Macrophage Extracellular Trap Formation via CLOCK-WNT10B-PAD2/ROS Signaling. [Abstract]2026 Jun 10;74(22):17392-17404. PMID: 42207496 -
Curr Res Microb Sci
The lncRNA GAS5-encoded micropeptide facilitates influenza virus replication through modulation of the Wnt/β-catenin signaling pathway. [Abstract]2026 Jan 27:10:100559. PMID: 41657547 -
Biochem Pharmacol
Pharmacological enhancement of repolarization reserve in human induced pluripotent stem cells derived cardiomyocytes. [Abstract]2019 Nov;169:113608. PMID: 31465775 -
Stem Cells Transl Med
High-throughput screening in postimplantation haploid epiblast stem cells reveals Hs3st3b1 as a modulator for reprogramming. [Abstract]2021 May;10(5):743-755. PMID: 33511777
IWP-2 purchased from MedChemExpress. Usage Cited in: Stem Cells Transl Med. 2021 May;10(5):743-755. [Abstract]
A schematic overview of the establishment of haEpiSCs from mouse post-implantation epiblast. Newly sorted haploid p53-KO haESCs were injected into the blastocysts. The reconstructed embryos were transferred to the oviducts of pseudopregnant CD-1 mice at 0.5 day.p.c, and subsequently developed to E6.5 stage for the establishment of haEpiSCs. Factors and inhibitors including activin A, bFGF and IWP-2 (2 μM) were added into the medium.
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Cell Rep Methods
2024 May 8:100777. PMID: 38744289 -
iScience
Otic organoids: A model to study spiral ganglion neuron characteristics in Tmprss3-deficiency. [Abstract]2025 Dec 5;29(1):114355. PMID: 41509903 -
J Inflamm Res
Early-Life Stress Induced by Neonatal Maternal Separation Leads to Intestinal 5-HT Accumulation and Causes Intestinal Dysfunction. [Abstract]2024 Nov 19:17:8945-8964. PMID: 39588137 -
J Cell Physiol
Wnt signaling associated small molecules improve the viability of pPSCs in a PI3K/Akt pathway dependent way. [Abstract]2020 Jul;235(7-8):5811-5822. PMID: 32003013 -
J Gerontol A Biol Sci Med Sci
2026 Jun 2:glag145. PMID: 42226012 -
Bioengineering (Basel)
Integrated Manufacturing of Suspended and Aligned Nanofibrous Scaffold for Structural Maturation and Synchronous Contraction of HiPSC-Derived Cardiomyocytes. [Abstract]2023 Jun 9;10(6):702. PMID: 37370633 -
Microb Pathog
2024 Sep 21:106960. PMID: 39313132 -
Exp Cell Res
Up-regulation of Dsg2 confered stem cells with malignancy through wnt/β-catenin signaling pathway. [Abstract]2022 Nov 11;422(1):113416. PMID: 36375513 -
Autoimmunity
2023 Dec;56(1):2182741. PMID: 36852641 -
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eNeuro
MicroRNA-155 Inhibition Activates Wnt/β-Catenin Signaling to Restore Th17/Treg Cell Balance and Protect against Acute Ischemic Stroke. [Abstract]2025 Jan 9:ENEURO.0347-24.2024. PMID: 39788733 -
PLoS One
Identification and characterization of two novel KCNH2 mutations contributing to long QT syndrome. [Abstract]2024 Jan 5;19(1):e0287206. PMID: 38181028 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198 -
Exp Ther Med
Inhibition of Rho-associated protein kinase improves the survival of human induced pluripotent stem cell-derived cardiomyocytes after dissociation. [Abstract]2020 Mar;19(3):1701-1710. PMID: 32104223 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
Solvente y solubilidad
DMF : 12.5 mg/mL (26.79 mM; ultrasonic and warming and heat to 60°C)
DMSO : 2 mg/mL (4.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.2 mg/mL (0.43 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (21.43 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
The human RCC cell lines 786O and Caki-2 (5×103) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20 μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490 nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. [Content Brief]
[2]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. [Content Brief]
[3]. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMF | 1 mM | 2.1432 mL | 10.7158 mL | 21.4316 mL | 53.5791 mL |
| DMF | 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL | 10.7158 mL |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL | 5.3579 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4288 mL | 3.5719 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0716 mL | 2.6790 mL | |
| 25 mM | 0.0857 mL | 0.4286 mL | 0.8573 mL | 2.1432 mL |
IWP-2 Related Classifications
HY-13912 Related Classifications
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