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SMI-16a
🥰Excellent
Catalog No. T3989Cas No. 587852-28-6
Alias PIM1/2 Kinase Inhibitor VI
SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).
SMI-16a
🥰Excellent
Purity: 99.05%
Catalog No. T3989Alias PIM1/2 Kinase Inhibitor VICas No. 587852-28-6
SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 2 mg | $40 | In Stock | |
| 5 mg | $64 | In Stock | |
| 10 mg | $89 | In Stock | |
| 25 mg | $163 | In Stock | |
| 50 mg | $247 | In Stock | |
| 100 mg | $372 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $84 | In Stock |
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Pim-1/2 kinase inhibitor 1
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Pim-1/2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].
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CK2/ERK8-IN-1
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T108271085822-09-8In house
CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).
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M-110
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M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases, showing a preference for PIM-3 (IC50=47 nM), and inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 also inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
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K00135
K-00135, K 00135, IMIDAZOPYRIDAZIN 1, Imidazol[1,2-b]pyridazine 1
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K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics.
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Pim-1 kinase inhibitor 4
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Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.
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Pim-1 kinase inhibitor 8
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XL413 hydrochloride
BMS-863233 Hydrochloride
T67352062200-97-7
XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 hydrochloride also exhibits potent effect with IC 50 s of 215, 42 nM on CK2, PIM1, respectively, and an EC 50 of 118 nM on pMCM.
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(Z)-SMI-4a
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(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.
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XL413 HCl
XL413 hydrochloride, BMS-863233 HCl
T713391169562-71-3
XL413 HCl is an ATP-competitive Cdc7 inhibitor (IC50: 3.4 nM) that is potent and selective.XL413 HCl inhibited CK2 and PIM1 with IC50 values of 215 and 42 nM, respectively.XL413 HCl showed an EC50 value of 118 against pMCM.
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CX-6258 hydrochloride
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Purity:99.05%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM). |
| Targets&IC50 | Pim1:150 nM, Pim2:20 nM |
| In vitro | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in PC3 human prostate cancer cultures in vitro (IC50: 48 μM). |
| In vivo | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20; 50 mg/kg/day, i.p.). |
| Kinase Assay | Competition binding reactions used 25 μg human M1 CHO membrane protein, BQCA or vehicle, and 0.15 nM [3H]NMS in 96-well deep-well plates. Binding reactions (30 °C for 2-3 h) are terminated by rapid filtration. Nonspecific binding is determined by adding 10 μM atropine. Filter plates are ished 4×with ice-cold 20 mM HEPES, 100 mM NaCl, and 5 mM MgCl2, pH 7.4 using a 96-well harvester. Plates are dried and radioactivity counted with a microplate scintillation counter[1]. |
| Alias | PIM1/2 Kinase Inhibitor VI |
| Molecular Weight | 263.31 |
| Formula | C13H13NO3S |
| Cas No. | 587852-28-6 |
| Smiles | CCCOc1ccc(\C=C2\SC(=O)NC2=O)cc1 |
| Relative Density. | 1.303 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (569.67 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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