JAK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/JAK.html JAKJanus kinaseJanus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via theJAK-STAT pathway. Since members of the type I and type II cytokine receptor families possess no catalytic kinas

2、e activity, they relyon the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transductionpathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associatewith a proline-rich regi

3、on in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. Afterthe receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs closeenough to phosphorylate each other. The JAK autophosphorylation

4、 induces a conformational change within itself, enabling it totransduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATsdissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate

5、 transcription of selectedgenes.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/JAK.html JAK HYPERLINK https:/www.MedChemE/Targets/JAK.html HYPERLINK https:/www.MedChemE/Targets/JAK.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/JAK.html HYPERLINK https:/www.MedChemE/Targets/JAK.html Ac

6、tivators HYPERLINK https:/www.MedChemE/Targets/JAK.html HYPERLINK https:/www.MedChemE/Targets/JAK.html & HYPERLINK https:/www.MedChemE/Targets/JAK.html HYPERLINK https:/www.MedChemE/Targets/JAK.html Agonists HYPERLINK https:/www.MedChemE/2r-5s-ritlecitinib.html (2R,5S)-Ritlecitinib(2R,5S)-PF-0665160

7、0) Cat. No.: HY-100754B HYPERLINK https:/www.MedChemE/_3R,4S_-Tofacitinib.html (3R,4S)-TofacitinibCat. No.: HY-40354D(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is apotent and selective JAK3 inhibitor (IC =144.850nM) extracted from patent US20150158864A1, example68.(3R,4S)-Tofacitinib is an less activ

8、e enantiomerof Tofacitinib. Tofacitinib inhibits JAK3 withIC of 1 nM.50Purity: 98.83%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/_3S,4R_-Tofacitinib.html (3S,4R)-Tofacitinib HYPERLINK https:/www.MedChemE/_3S,4R_-Tof

9、acitinib.html HYPERLINK https:/www.MedChemE/_3S,4S_-Tofacitinib.html (3S,4S)-TofacitinibCat. No.: HY-40354B Cat. No.: HY-40354C(3S,4R)-Tofacitinib is an less active enantiomerof Tofacitinib. Tofacitinib inhibits JAK3 withIC of 1 nM.50(3S,4S)-Tofacitinib is the less activeS-enantiomer of Tofacitinib.

10、 Tofacitinib inhibitsJAK3 with IC of 1 nM.50Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.24%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/e-z-ag490.html (E/Z)-AG490(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42) Cat. No.: HY-107459 HYPERLINK https:/www.

11、MedChemE/SB1317.html (E/Z)-Zotiraciclib(E/Z)-TG02; (E/Z)-SB1317) Cat. No.: HY-15166(E/Z)-AG490 (E/Z)-Tyrphostin AG490) is a racemiccompound of (E)-AG490 and (Z)-AG490 isomers.(E)-AG490 (HY-12000) is a tyrosine kinase inhibitorthat inhibits EGFR, Stat-3 and JAK2/3.(E/Z)-Zotiraciclib (E/Z)-TG02) is a

12、potentinhibitor of CDK2, JAK2, and FLT3.(E/Z)-Zotiraciclib (E/Z)-TG02) can be used forthe research of cancer.Purity: 96.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.96%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/e-z-zotiracic

13、lib-citrate.html (E/Z)-Zotiraciclib HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-citrate.html HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-citrate.html citrate HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-citrate.html HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-hydrochloride.html (E/Z)-Zoti

14、raciclib HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-hydrochloride.html HYPERLINK https:/www.MedChemE/e-z-zotiraciclib-hydrochloride.html hydrochloride(E/Z)-TG02 citrate; (E/Z)-SB1317 citrate) Cat. No.: HY-15166B (E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride) Cat. No.: HY-15166A(E/Z)-Zotir

15、aciclib citrate is a potent CDK2,JAK2, and FLT3 inhibitor.(E/Z)-Zotiraciclib (E/Z)-TG02) hydrochloride is apotent CDK2, JAK2, and FLT3 inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.45%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPER

16、LINK https:/www.MedChemE/rac-ruxolitinib-d9.html (Rac)-Ruxolitinib-d9 HYPERLINK https:/www.MedChemE/rac-ruxolitinib-d9.html HYPERLINK https:/www.MedChemE/gdc-046.html 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benz(Rac)-INCB18424-d9) Cat. No.: HY-W062703S HYPERLINK https:/www.MedChemE/g

17、dc-046.html amide HYPERLINK https:/www.MedChemE/gdc-046.html Cat. No.: HY-120469(Rac)-Ruxolitinib D9 (Rac)-INCB18424 D9) is thedeuterium labeled (Rac)-Ruxolitinib.(Rac)-Ruxolitinib is a JAK2 inhibitor.GDC-046 is a potent, selective, and orallybioavailable TYK2 inhibitor with Ks of 4.8, 0.7,i0.7, and

18、 0.4 nM for TYK2, JAK1, JAK2, and JAK3,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Abroci

19、tinib.html Abrocitinib(PF-04965842) Cat. No.: HY-107429 HYPERLINK https:/www.MedChemE/AG-490.html AG490(Tyrphostin AG490; Tyrphostin B42) Cat. No.: HY-12000Abrocitinib (PF-04965842) is a potent, orallyactive and selective JAK1 inhibitor, with IC s50of 29 and 803 nM for JAK1 and JAK2, respectively.AG

20、490 (Tyrphostin AG490) is a tyrosine kinaseinhibitor that inhibits EGFR, Stat-3 andJAK2/3.Purity: 99.26%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.Me

21、dChemE/AMG-47a.html AMG-47a HYPERLINK https:/www.MedChemE/AMG-47a.html HYPERLINK https:/www.MedChemE/at9283.html AT9283Cat. No.: HY-18303 Cat. No.: HY-50514AMG-47a is a potent and orally activelymphocyte-specific protein tyrosine kinase(Lck) inhibitor, with an IC of 0.2 nM. AMG-47a50also inhibits VE

22、GF2, p38, Jak3 and MLR andIL-2 with IC s of 1 nM, 3 nM, 72 nM, 30 nM and 2150nM, respectively.AT9283 is a multi-targeted kinase inhibitor withpotent activity against Aurora A/B, JAK2/3, Abl(T315I) and Flt3 (IC s ranging from 1 to 30 nM).50AT9283 inhibits growth and survival of multiplesolid tumors i

23、n vitro and in vivo.Purity: 98.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.70%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Atractylenolide-I.html Atractylenolide HYPERLINK https:/www.MedChemE

24、/Atractylenolide-I.html HYPERLINK https:/www.MedChemE/Atractylenolide-I.html I HYPERLINK https:/www.MedChemE/Atractylenolide-I.html HYPERLINK https:/www.MedChemE/AZ-3.html AZ-3Cat. No.: HY-N0201 Cat. No.: HY-112442Atractylenolide I is a sesquiterpene derived fromthe rhizome of Atractylodes macroceph

25、ala,possesses diverse bioactivities, such asneuroprotective, anti-allergic, anti-inflammatoryand anticancer properties.AZ-3 is a potent and selective JAK1 inhibitorwith an IC of 34 nM.50Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data:

26、No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZ960.html AZ960 HYPERLINK https:/www.MedChemE/AZ960.html HYPERLINK https:/www.MedChemE/AZD-1480.html AZD-1480Cat. No.: HY-10411 Cat. No.: HY-10193AZ960 is a potent and specific inhibitor of theJAK2 kinase with a K of 0.45 nM.iAZD

27、-1480 is an ATP-competitive inhibitor of JAK1and JAK2 with IC s of 1.3 nM and5098%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bd750.html BD750 HYPERLINK https:/www.MedChemE/bd750.html HYPERLINK

28、https:/www.MedChemE/BMS-066.html BMS-066Cat. No.: HY-131140 Cat. No.: HY-18710BD750, an effective immunosuppressant and aJAK3/STAT5 inhibitor, inhibits IL-2-inducedJAK3/STAT5-dependent T cell proliferation, withIC values of 1.5 M and 1.1 M in mouse and human50T cells, respectively.BMS-066 is an IKK/

29、Tyk2 pseudokinase inhibitor,with IC s of 9 nM and 72 nM, respectively.50Purity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BMS-911543.html BMS-911543 HY

30、PERLINK https:/www.MedChemE/BMS-911543.html HYPERLINK https:/www.MedChemE/bms-986202.html BMS-986202Cat. No.: HY-15270 Cat. No.: HY-131968BMS-911543 is a selective JAK2 inhibitor, withIC s of 1.1 nM, less selective at JAK1, JAK3 and50TYK2 (IC , 75, 360, 66 nM, respectively).50BMS-986202 is a potent,

31、 selective and orallyactive Tyk2 inhibitor that binds to Tyk2 JH2with an IC of 0.19 nM and a of 0.02 nM.50 KiBMS-986202 is remarkably selective over otherkinases including Jak family members.Purity: 98.05%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.46%Clinical

32、Data: Phase 1Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/PF-06700841.html Brepocitinib HYPERLINK https:/www.MedChemE/PF-06700841.html HYPERLINK https:/www.MedChemE/PF-06700841_P-Tosylate.html Brepocitinib HYPERLINK https:/www.MedChemE/PF-06700841_P-Tosylate.html HYPERLINK h

33、ttps:/www.MedChemE/PF-06700841_P-Tosylate.html P-Tosylate(PF-06700841) Cat. No.: HY-112708 (PF-06700841 P-Tosylate) Cat. No.: HY-112708ABrepocitinib (PF-06700841) is a potent dualJanus kinase 1 (JAK1) and TYK2 inhibitor withIC s of 17 nM and 23 nM, respectively.50Brepocitinib also inhibits JAK2 and

34、JAK3 withIC s of 77 nM and 6.49 M, respectively.50Brepocitinib (PF-06700841) P-Tosylate is a potentdual Janus kinase 1 (JAK1) and TYK2 inhibitorwith IC s of 17 nM and 23 nM, respectively.50Brepocitinib P-Tosylate also inhibits JAK2 andJAK3 with IC s of 77 nM and 6.49 M,50respectively.Purity: 98%Clin

35、ical Data: Phase 2Size: 1 mg, 5 mgPurity: 99.69%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/brevilin-a.html Brevilin HYPERLINK https:/www.MedChemE/brevilin-a.html HYPERLINK https:/www.MedChemE/brevilin-a.html A HYPERLINK https:/www.MedChemE/brevil

36、in-a.html HYPERLINK https:/www.MedChemE/cep-1347.html CEP-1347Cat. No.: HY-N2959(KT7515) Cat. No.: HY-10412Brevilin A is a sesquiterpene lactone isolatedfrom Centipeda minima with anti-tumor activity.Brevilin A is a selective inhibitor of JAK-STATsignal pathway by attenuating the JAKs activityand bl

37、ocking STAT3 signaling (IC =10.6 M) in50Cancer Cells.CEP-1347 is an inhibitor of the JNK/SAPK pathwaywith neuroprotective effects.Purity: 99.77%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Emai

38、l: salesMedChemE HYPERLINK https:/www.MedChemE/CEP-33779.html CEP-33779Cat. No.: HY-15343 HYPERLINK https:/www.MedChemE/Cerdulatinib.html Cerdulatinib(PRT062070; PRT2070) Cat. No.: HY-15999CEP-33779 is a novel, selective, and orallybioavailable inhibitor of JAK2 with an IC of501.80.6 nM.Cerdulatinib

39、 (PRT062070) is a selective Tyk2inhibitor with an IC of 0.5 nM. Cerdulatinib50(PRT062070) also is a dual JAK and SYK inhibitorwith IC s of 12, 6, 8 and 32 for JAK1, 2, 3 and50SYK, respectively.Purity: 99.36%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.

40、0%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/cerdulatinib-hydrochloride.html Cerdulatinib HYPERLINK https:/www.MedChemE/cerdulatinib-hydrochloride.html HYPERLINK https:/www.MedChemE/cerdulatinib-hydrochloride.html hydrochloride(PRT062070

41、hydrochloride; PRT2070 hydrochloride) Cat. No.: HY-15999A HYPERLINK https:/www.MedChemE/CHZ868.html CHZ868Cat. No.: HY-18960Cerdulatinib hydrochloride (PRT062070) is aselective, oral active and reversibleATP-competitive inhibitor of dual SYK and JAK,with IC s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM50

42、for SYK and Tyk2, JAK1, 2, 3, respectively.CHZ868 is a type II JAK2 inhibitor with an IC50of 0.17 M in EPOR JAK2 WT Ba/F3 cell.Purity: 99.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 1

43、0 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/coumermycin-a1.html Coumermycin HYPERLINK https:/www.MedChemE/coumermycin-a1.html HYPERLINK https:/www.MedChemE/coumermycin-a1.html A1Cat. No.: HY-N7452 HYPERLINK https:/www.MedChemE/Cucurbitacin-I.html Cucurbitacin HYPERLINK https:/www.MedChe

44、mE/Cucurbitacin-I.html HYPERLINK https:/www.MedChemE/Cucurbitacin-I.html I(Elatericin B; JSI-124; NSC-521777) Cat. No.: HY-N1405Coumermycin A1 is a JAK2 signal activator.Coumermycin A1 inhibits DNA Gyrase which therebyinhibits cell division in bacteria.Cucurbitacin I is a natural selective inhibitor

45、 ofJAK2/STAT3, with potent anti-cancer activity.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/curculigoside.html Curculigoside HYPERLINK https:/www.MedChemE/curculigosi

46、de.html HYPERLINK https:/www.MedChemE/debio-0617b.html Debio HYPERLINK https:/www.MedChemE/debio-0617b.html HYPERLINK https:/www.MedChemE/debio-0617b.html 0617BCat. No.: HY-N0705 Cat. No.: HY-108417Curculigoside is the main saponin in C. orchioide,exerts significant antioxidant, anti-osteoporosis,an

47、tidepressant and neuroprotection effects.Curculigoside possesses significant anti-arthriticeffects in vivo and in vitro via regulation of theJAK/STAT/NF-B signaling pathway.Debio 0617B, a multi-kinase inhibitor, reducesmaintenance and self-renewal of primary human AMLCD34+ stem/progenitor cells.Puri

48、ty: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Decernotinib.html Decernotinib HYPERLINK https:/www.MedChemE/Decernotinib.html HYPERLINK https:/www.MedChemE/dehydrocrena

49、tidine.html Dehydrocrenatidine(VX-509; VRT-831509) Cat. No.: HY-12469 (Kumujian G; O-Methylpicrasidine I) Cat. No.: HY-N3710Decernotinib is a potent, orally active JAK3inhibitor, with Ks of 2.5, 11, 13 and 11 nM foriJAK3, JAK1, JAK2, and TYK2, respectively.Dehydrocrenatidine, a natural alkaloid, is

50、aspecific JAK inhibitor. Dehydrocrenatidineinhibits voltage-gated sodium channels andameliorates mechanic allodia in a rat model ofneuropathic pain.Purity: 99.67%Clinical Data: Phase 3Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg,

51、 25 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/Delgocitinib.html Delgocitinib(JTE-052) Cat. No.: HY-109053 HYPERLINK https:/www.MedChemE/delphinidin-chloride.html Delphinidin HYPERLINK https:/www.MedChemE/delphinidin-chloride.html HYPERLINK https:/www.MedChemE/delphinidin-chloride.html chlorideC

52、at. No.: HY-N2409Delgocitinib (JTE-052) is a specific JAKinhibitor with IC s of 2.8, 2.6, 13 and 58 nM for50JAK1, JAK2, JAK3 and Tyk2, respectively.Delphinidin chloride, an anthocyanidin, isisolated from berries and red wine. Delphinidinchloride shows endothelium-dependentvasorelaxation. Delphinidin

53、 chloride also canmodulate JAK/STAT3 and MAPKinase signaling toinduce apoptosis in HCT116 cells.Purity: 99.76%Clinical Data: LaunchedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/BMS-986165.

54、html Deucravacitinib(BMS-986165) Cat. No.: HY-117287 HYPERLINK https:/www.MedChemE/deuterated-ruxolitinib.html Deuruxolitinib(CTP-543; Ruxolitinib D8; Deuterated Ruxolitinib) Cat. No.: HY-50856SDeucravacitinib (BMS-986165) is a highlyselective, orally bioavailable allosteric TYK2inhibitor for the tr

55、eatment of autoimmunediseases, which selectively binds to TYK2pseudokinase (JH2) domain (IC =1.0 nM) and blocks50receptor-mediated Tyk2 activation byDeuruxolitinib (CTP-543), a deuteratedRuxolitinib, modulates the activity of JAK1/JAK2.Deuruxolitinib can be used for the research hairloss disorders (

56、from patent WO2017192905A1,compound I).Purity: 99.79%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dtp3.html DTP3Cat. No.: HY-100538 HYPERLINK https:/www.MedChemE/TG-101

57、348.html Fedratinib(TG-101348; SAR 302503) Cat. No.: HY-10409DTP3 TFA is a potent and selective GADD45/MKK7inhibitor. DTP3 TFA targets an essential,cancer-selective cell-survival module downstreamof the NF-B pathway.Fedratinib (TG-101348) is a potent, selective,ATP-competitive and orally active JAK2

58、 inhibitorwith IC50s of 3 nM for both JAK2 and JAK2V617Fkinase. Fedratinib shows 35- and 334-foldselectivity over JAK1 and JAK3, respectively.Purity: 99.43%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.87%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg,

59、 100 mg, 200 mg, 500 mg, 1 g HYPERLINK https:/www.MedChemE/fedratinib-hydrochloride-hydrate.html Fedratinib HYPERLINK https:/www.MedChemE/fedratinib-hydrochloride-hydrate.html HYPERLINK https:/www.MedChemE/fedratinib-hydrochloride-hydrate.html hydrochloride HYPERLINK https:/www.MedChemE/fedratinib-h

60、ydrochloride-hydrate.html HYPERLINK https:/www.MedChemE/fedratinib-hydrochloride-hydrate.html hydrate HYPERLINK https:/www.MedChemE/fedratinib-hydrochloride-hydrate.html (TG-101348 hydrochloride HYPERLINK https:/www.MedChemE/GLPG0634.html Filgotinibhydrate; SAR 302503 hydrochloride hydrate) Cat. No.