MedKoo Cat#: 407145 | Name: WHI-P131
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

WHI-P131, also known as Janex 1, is a potent and selective Janus kinase 3 inhibitor with an IC50 value of 78 µM. WHI-P131 inhibits human glioblastoma cell adhesion and invasion. WHI-P131 prevents graft-versus-host disease but spares the graft-versus-leukemia function of the bone marrow allografts in a murine bone marrow transplantation model.

Chemical Structure

WHI-P131
WHI-P131
CAS#202475-60-3

Theoretical Analysis

MedKoo Cat#: 407145

Name: WHI-P131

CAS#: 202475-60-3

Chemical Formula: C16H15N3O3

Exact Mass: 297.1113

Molecular Weight: 297.31

Elemental Analysis: C, 64.64; H, 5.09; N, 14.13; O, 16.14

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 2 Weeks
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,250.00 2 Weeks
1g USD 1,950.00 2 Weeks
2g USD 2,950.00 2 Weeks
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Synonym
WHI-P131, WHI P-131, WHI P131, Janex 1
IUPAC/Chemical Name
4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
InChi Key
HOZUXBLMYUPGPZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-3-5-11(20)6-4-10/h3-9,20H,1-2H3,(H,17,18,19)
SMILES Code
OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1
Appearance
White to off-white crystalline powder.
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 297.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Jo WT, Kim AY, Woo HG, Song HJ, Baik EJ. Effect of Janus Kinase 3 Inhibitor on Sebaceous Gland Regeneration during Skin Wound Healing. Ann Dermatol. 2023 Aug;35(4):275-284. doi: 10.5021/ad.22.204. PMID: 37550228; PMCID: PMC10407337. 2: Pan L, Peng Z, Zhang R, Zhang R, Liang D, Chen H, Tian H. JANEX-1 improves acute pulmonary embolism through VEGF and FAK in pulmonary artery smooth muscle cells. Exp Biol Med (Maywood). 2020 Sep;245(15):1395-1403. doi: 10.1177/1535370220942474. Epub 2020 Jul 15. Erratum in: Exp Biol Med (Maywood). 2021 Jan;246(2):NP1. doi: 10.1177/1535370220976078. PMID: 32664806; PMCID: PMC7441354. 3: Güven DC, Orhan C, Şahin K, Uçkun FM. Data-Driven identification of chemopreventive agents for breast cancer. Turk J Med Sci. 2020 Nov 3;50(SI-2):1691-1696. doi: 10.3906/sag-2003-138. PMID: 32233182; PMCID: PMC7672343. 4: Sahin K, Yabas M, Orhan C, Tuzcu M, Sahin TK, Ozercan IH, Qazi S, Uckun FM. Prevention of DMBA-induced mammary gland tumors in mice by a dual-function inhibitor of JAK3 and EGF receptor tyrosine kinases. Expert Opin Ther Targets. 2020 Apr;24(4):379-387. doi: 10.1080/14728222.2020.1737014. Epub 2020 Mar 2. PMID: 32106727. 5: Meszaros EC, Malemud CJ. Phosphorylation of STAT proteins by recombinant human IL-6 in immortalized human chondrocyte cell lines, T/C28a2 and C28/I2. J Inflamm Res. 2017 Sep 28;10:143-150. doi: 10.2147/JIR.S93797. PMID: 29026328; PMCID: PMC5627728. 6: Wang YC, Cui XB, Chuang YH, Chen SY. Janus Kinase 3, a Novel Regulator for Smooth Muscle Proliferation and Vascular Remodeling. Arterioscler Thromb Vasc Biol. 2017 Jul;37(7):1352-1360. doi: 10.1161/ATVBAHA.116.308895. Epub 2017 May 4. PMID: 28473442; PMCID: PMC5503700. 7: Shatrova AN, Mityushova EV, Vassilieva IO, Aksenov ND, Zenin VV, Nikolsky NN, Marakhova II. Time-Dependent Regulation of IL-2R α-Chain (CD25) Expression by TCR Signal Strength and IL-2-Induced STAT5 Signaling in Activated Human Blood T Lymphocytes. PLoS One. 2016 Dec 9;11(12):e0167215. doi: 10.1371/journal.pone.0167215. PMID: 27936140; PMCID: PMC5172478. 8: Bhavsar SK, Singh Y, Sharma P, Khairnar V, Hosseinzadeh Z, Zhang S, Palmada M, Sabolic I, Koepsell H, Lang KS, Lang PA, Lang F. Expression of JAK3 Sensitive Na+ Coupled Glucose Carrier SGLT1 in Activated Cytotoxic T Lymphocytes. Cell Physiol Biochem. 2016;39(3):1209-28. doi: 10.1159/000447827. Epub 2016 Sep 5. PMID: 27595398. 9: Shatrova AN, Mityushova EV, Aksenov NV, Marakhova LL. [THE INDUCTION OF CD25 EXPRESSION IN Jurkat T CELLS]. Tsitologiia. 2015;57(5):345-52. Russian. PMID: 26281211. 10: Oh YB, Ahn M, Lee SM, Koh HW, Lee SH, Kim SH, Park BH. Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice. Exp Mol Med. 2013 May 17;45(5):e23. doi: 10.1038/emm.2013.43. PMID: 23680658; PMCID: PMC3674406. 11: Mitiushova EV, Shatrova AN, Zenin VV, Aksenov ND, Marakhova II. [The STAT5 signaling in the expression of alpha-subunit of interleukin-2 receptor in human blood lymphocytes]. Tsitologiia. 2013;55(6):421-9. Russian. PMID: 25509109. 12: Cetkovic-Cvrlje M, Olson M, Ghate K. Targeting Janus tyrosine kinase 3 (JAK3) with an inhibitor induces secretion of TGF-β by CD4+ T cells. Cell Mol Immunol. 2012 Jul;9(4):350-60. doi: 10.1038/cmi.2012.20. Epub 2012 Jun 25. PMID: 22728763; PMCID: PMC4012866. 13: Chiba Y, Goto K, Misawa M. Interleukin-13-induced activation of signal transducer and activator of transcription 6 is mediated by an activation of Janus kinase 1 in cultured human bronchial smooth muscle cells. Pharmacol Rep. 2012;64(2):454-8. doi: 10.1016/s1734-1140(12)70788-0. PMID: 22661199. 14: Lee JE, Lee AS, Kim DH, Jung YJ, Lee S, Park BH, Lee SH, Park SK, Kim W, Kang KP. Janex-1, a JAK3 inhibitor, ameliorates tumor necrosis factor-α-induced expression of cell adhesion molecules and improves myocardial vascular permeability in endotoxemic mice. Int J Mol Med. 2012 May;29(5):864-70. doi: 10.3892/ijmm.2012.920. Epub 2012 Feb 16. PMID: 22344597. 15: Aida Y, Honda K, Tanigawa S, Nakayama G, Matsumura H, Suzuki N, Shimizu O, Takeichi O, Makimura M, Maeno M. IL-6 and soluble IL-6 receptor stimulate the production of MMPs and their inhibitors via JAK-STAT and ERK-MAPK signalling in human chondrocytes. Cell Biol Int. 2012 Apr 1;36(4):367-76. doi: 10.1042/CBI20110150. PMID: 22087578. 16: Shatrova AN, Zenin VV, Aksenov ND, Mitiushova EV, Marakhova II. [The surface expression of CD25 at different stages of proliferative response in human lymphocytes. II. The role of interleukin-2]. Tsitologiia. 2011;53(8):652-8. Russian. PMID: 21961284. 17: Zenin VV, Aksenov ND, Shatrova AN, Mitiushova EV, Marakhova II. [The surface expression of CD25 at different stages of proliferative response in human lymphocytes. I. The role of JAK and Src tyrosine kinases as revealed by inhibitory analysis]. Tsitologiia. 2011;53(8):645-51. Russian. PMID: 21961283. 18: Bhavsar SK, Gu S, Bobbala D, Lang F. Janus kinase 3 is expressed in erythrocytes, phosphorylated upon energy depletion and involved in the regulation of suicidal erythrocyte death. Cell Physiol Biochem. 2011;27(5):547-56. doi: 10.1159/000329956. Epub 2011 Jun 15. PMID: 21691072. 19: Batista A, Barata JT, Raderschall E, Sallan SE, Carlesso N, Nadler LM, Cardoso AA. Targeting of active mTOR inhibits primary leukemia T cells and synergizes with cytotoxic drugs and signaling inhibitors. Exp Hematol. 2011 Apr;39(4):457-472.e3. doi: 10.1016/j.exphem.2011.01.005. Epub 2011 Jan 26. PMID: 21277936. 20: Uckun FM, Dibirdik I. Chemoprevention of colorectal cancer by targeting Janus kinase 3 with a rationally designed small molecule inhibitor. Nutr Cancer. 2010;62(7):968-72. doi: 10.1080/01635581.2010.513471. PMID: 20924972.