Momelotinib mesylate
Based on 18 publication(s) in Google Scholar
Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
For research use only. We do not sell to patients.
- CAS No.: 1056636-07-7
- Formula: C24H26N6O5S
- Molecular Weight:510.57
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Momelotinib mesylate
More- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Cell. 2018 Sep 10;34(3):439-452.e6. [Abstract]
- Cancer Res. 2020 Jan 1;80(1):44-56. [Abstract]
- Nat Commun. 2025 Jul 24;16(1):6777. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Leukemia. 2012 Oct;26(10):2233-44. [Abstract]
- Metabolism. 2025 Apr 4:156259. [Abstract]
- Int J Biol Sci. 2022 Jan 1;18(2):585-598. [Abstract]
- Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
- Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Pineal Res. 2019 Apr;66(3):e12552. [Abstract]
- J Enzyme Inhib Med Chem. 2025 Dec;40(1):2488127. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- J Clin Lab Anal. 2026 Feb;40(4):e70161. [Abstract]
- Immunol Invest. 2022 Aug;51(6):1582-1597. [Abstract]
- Environ Monit Assess. 2025 Apr 10;197(5):533. [Abstract]
- bioRxiv. 2025 Oct 25.
Customer Validation & Images
-
WB
-
RT-PCR
-
IF
-
WB
-
ELISA
Biological Activity
|
JAK1 11 nM (IC50) |
JAK2 18 nM (IC50) |
JAK3 155 nM (IC50) |
Momelotinib mesylate is an inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. Momelotinib inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, Momelotinib also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, Momelotinib has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2 μM-4 μM[1]. Momelotinib inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) 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
-
CAS No. 1056636-07-7
-
Molecular Weight 510.57
-
Formula C24H26N6O5S
-
SMILES
O=C(C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1)NCC#N.O=S(O)(C)=O
-
Synonyms
CYT387 mesylate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
-
Cancer Cell
2018 Sep 10;34(3):439-452.e6. PMID: 30205046
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Sep 10;34(3):439-452.e6. [Abstract]
Immunoblot (IB) of the indicated proteins in A549, H2009, HCC44, and H1792 cells treated with indicated concentration of Momelotinib (MMB) for 24 hr.
-
Cancer Res
Phosphorylation of RAB7 by TBK1/IKKε Regulates Innate Immune Signaling in Triple-Negative Breast Cancer. [Abstract]2020 Jan 1;80(1):44-56. PMID: 31662325
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jan 1;80(1):44-56. [Abstract]
Immunofluorescence imaging of parental and Rab7 cell lines: WT, S72E, and S72A, treated with either 1 μM Compound 1 (6 h), 5 μM MRT67307 (8 h) or 5 μM Momelotinib (CYT387) (3 h) alone (representative, n=2; scale=10μm).
-
Nat Commun
PEAK1 maintains tight junctions in intestinal epithelial cells and resists colitis by inhibiting autophagy-mediated ZO-1 degradation. [Abstract]2025 Jul 24;16(1):6777. PMID: 40707483 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Leukemia
Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. [Abstract]2012 Oct;26(10):2233-44. PMID: 22469781 -
Metabolism
Propagation of senescent phenotypes by extracellular HMGB1 is dependent on its redox state. [Abstract]2025 Apr 4:156259. PMID: 40189139 -
Int J Biol Sci
Rocaglamide promotes the infiltration and antitumor immunity of NK cells by activating cGAS-STING signaling in non-small cell lung cancer. [Abstract]2022 Jan 1;18(2):585-598. PMID: 35002511
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2022 Jan 1;18(2):585-598. [Abstract]
A549, H1299, H1975, and LLC cells were treated with or without 25 nM of RocA in the presence or absence of 5 µM Momelotinib (CYT387), or 10 µM BAY11 for 24 h, and then the expressions of CCL5 and CXCL10 were analyzed by real-time PCR.
-
Cell Death Dis
4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]2022 Dec 27;13(12):1075. PMID: 36575176
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
A549 cells transfected with either control siRNA or 4EBP1 siRNAs were treated with Momelotinib (CYT387) or LY3214996 for 10 h in normal or glucose starvation conditions. Western blot analysis of p-STAT3 (Y705) expression. The results showed that CYT387 and LY3214996 could inhibit the phosphorylation of STAT3. Furthermore, the increased protein levels of p-STAT3 by knocking down 4EBP1 under GS were attenuated when treating with CYT387 or LY3214996 in A549 cells.
-
Cancer Immunol Res
2016 Jun;4(6):520-30. PMID: 27068336
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
CCL5 ELISA in 8988T-sgATG5 cells 24 h after a 60 min IL1β pulse ± 2.5 μM Momelotinib (CYT387) or ruxolitinib, mean and SD of duplicate samples shown.
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
H&E staining and IHC for CCL5, p62 or PD-L1 in pancreatic tissue harvested from C57/BL6 mice pretreated with vehicle control or daily Momelotinib (CYT387, 50 mg/kg; i.g.) day 1 post-cerulein. The results showed that CYT387 significantly inhibited the expression of CCL5 and PD-L1.
Momelotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
Inflammatory cell infiltration in pancreatic tissue from 3 random sites (200x) following vehicle (n = 4) or Momelotinib (CYT387, 50 mg/kg; i.g.; once daily for 2 days) (n = 2) treatment. Mean and SEM shown, P value calculated by Student t-test. The results demonstrated that CYT387 markedly reduced inflammatory cell infiltration following lanserin stimulation.
-
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Pineal Res
MicroRNA-7 inhibits melatonin synthesis by acting as a linking molecule between leptin and norepinephrine signaling pathways in pig pineal gland. [Abstract]2019 Apr;66(3):e12552. PMID: 30618087 -
J Enzyme Inhib Med Chem
Discovery and biological evaluation of a novel and highly potent JAK2 inhibitor for the treatment of triple negative breast cancer. [Abstract]2025 Dec;40(1):2488127. PMID: 40298145 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
J Clin Lab Anal
The Immunoregulatory and Hematopoietic Effects of Momelotinib in a Murine Bone Marrow Failure Model. [Abstract]2026 Feb;40(4):e70161. PMID: 41552919 -
Immunol Invest
CYT387 Inhibits the Hyperproliferative Potential of Fibroblast-like Synoviocytes via Modulation of IL-6/JAK1/STAT3 Signaling in Rheumatoid Arthritis. [Abstract]2022 Aug;51(6):1582-1597. PMID: 34704880 -
Environ Monit Assess
Assessment of the physicochemical characteristics of by-products of cassava processing and their effects on biodiversity. [Abstract]2025 Apr 10;197(5):533. PMID: 40208441 -
Protocol
Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37°C with 5% CO2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
On day 32 after bone marrow transplantation (when all mice exhibit severe leukocytosis and erythrocytosis), mice are assigned to 3 groups such that each group had equivalent average body weight and blood counts. Momelotinib is dissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone). Subsequently, the Momelotinib/NMP mix is diluted with 0.14 M Captisol to a concentration of 6 mg/mL and further diluted with 0.1 M Captisol to a final concentration of 4 mg/mL. All 3 groups of mice (n=12 per group) are administered Momelotinib by oral gavage twice daily at 10- to 12-hour intervals from day 34 after bone marrow transplantation to day 82 (end of experiment). Mice receive NMP/Captisol without Momelotinib (0 mg/kg group), 25 mg/kg Momelotinib, or 50 mg/kg Momelotinib. At day 82 after bone marrow transplantation, all mice are euthanized for analysis except for 2 mice each from the 50 mg/kg and 25 mg/kg groups, which are taken off Momelotinib treatment and followed for 45 additional days. For assessment of the effects of Momelotinib on normal blood counts, naive Balb/c mice are administered vehicle control, or 50 mg/kg, or 100 mg/kg Momelotinib in an identical fashion for the bone marrow transplant experimental mouse cohort. Peripheral blood is drawn at day 14, 28, 42, and 56 and levels of red cells, white cells, reticulocytes, granulocytes, lymphocytes, and monocytes are analyzed[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. [Content Brief]
[2]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899. [Content Brief]
[3]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz