Shopping Cart
- Remove All
Your shopping cart is currently empty
FM-381
Catalog No. T5091Cas No. 2226521-65-7
Alias FM381
FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
FM-381
Catalog No. T5091Alias FM381Cas No. 2226521-65-7
FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $48 | In Stock | |
| 5 mg | $113 | In Stock | |
| 10 mg | $163 | In Stock | |
| 25 mg | $339 | In Stock | |
| 50 mg | $493 | In Stock | |
| 100 mg | $723 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $125 | In Stock |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "FM-381"
Ruxolitinib phosphate
Cited
Ruxolitinib (INCB-18424) phosphate, INCB018424 phosphate, INCB018424, INC424, INC 424 phosphate
T30431092939-17-7
Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1/2 inhibitor with IC50 of 3.3 nM/2.8 nM. Its selectivity for JAK1/2 is more than 130 times that of JAK3.
- $44
Size
QTY
CitedTofacitinib Citrate
Tofacitinib (CP-690550) Citrate, Tasocitinib citrate, CP-690550 citrate
T2398540737-29-9
Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
- $32
Size
QTY
Delgocitinib
JTE-052, Corectim（Delgocitinib）
T150961263774-59-9
Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.
- $172
Size
QTY
Ruxolitinib Cited
INCB018424, (R)-Ruxolitinib
T1829941678-49-5
Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
- $53
Size
QTY
CitedFedratinib Cited
TG-101348, SAR 302503
T1995936091-26-8
Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
- $45
Size
QTY
CitedDeucravacitinib
BMS-986165
T146871609392-27-9
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.
- $64
Size
QTY
Baricitinib Cited
LY3009104, INCB028050
T24851187594-09-7
Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.
- $43
Size
QTY
CitedTofacitinib Cited
Tasocitinib, CP-690550
T6321477600-75-2
Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.
- $30
Size
QTY
CitedRO8191 Cited
RO4948191, CDM-3008
T22142691868-88-9
RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
- $38
Size
QTY
CitedCEP-33779
Cited
CEP33779
T61221257704-57-6
CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
- $38
Size
QTY
CitedWHI-P97 Cited
T4657211555-05-4
WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.
- $44
Size
QTY
CitedSelect Batch
Purity:99.33%
Contact us for more batch information
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 | FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. |
| Targets&IC50 | JAK3:127 pM |
| In vitro | FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 μM [1]. |
| Cell Research | CD4+ T Cell cytokine stimulation assay is performed. T cells are purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells are incubated for 1 hr with JAK inhibitors (FM381) (0, 10, 50, 100, 300 nM) or DMSO control and stimulated with cytokines for 30 min. The cells are lysed, and the proteins are separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest are blotted with specific antibodies and visualized with an infrared imaging system[1]. |
| Alias | FM381 |
| Molecular Weight | 428.49 |
| Formula | C24H24N6O2 |
| Cas No. | 2226521-65-7 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | H2O: Insoluble DMSO: 12.5 mg/mL (29.17 mM)  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Calculator
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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy FM-381 | purchase FM-381 | FM-381 cost | order FM-381 | FM-381 chemical structure | FM-381 in vitro | FM-381 formula | FM-381 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.