TGF-β-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html TGF- HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html ReceptorTransforming growth factor beta receptorsTGF- receptors (Transforming growth factor- receptors) are single pass ser

2、ine/threonine kinase receptors. Transforming growthfactor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes,including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in b

3、oth normaland diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor,both serine/threonine kinases.The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transdu

4、ceTGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain,a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activatesdownstream signaling molecules. ALKs

5、mediate the effect of TGF-beta superfamily on a variety of cellular processes such asproliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes.Some ALKs have been implicated in several disorders, including tumorigenesis and imm

6、une diseases, suggesting that thesereceptors can be used as drug targets.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html TGF- HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html Receptor HYPERLINK https:/www.MedChe

7、mE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www

8、.MedChemE/Targets/TGF- Receptor.html Antagonists HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html & HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html HYPERLINK https:/www.MedChemE/Targets/TGF- Receptor.html Activators HYPERLINK

9、https:/www.MedChemE/a-77-01.html A HYPERLINK https:/www.MedChemE/a-77-01.html HYPERLINK https:/www.MedChemE/a-77-01.html 77-01 HYPERLINK https:/www.MedChemE/a-77-01.html HYPERLINK https:/www.MedChemE/A-83-01.html A HYPERLINK https:/www.MedChemE/A-83-01.html HYPERLINK https:/www.MedChemE/A-83-01.html

10、 83-01Cat. No.: HY-78349 Cat. No.: HY-10432A 77-01 is a potent inhibitor of transforminggrowth factor (TGF)- type I receptor superfamilyactivin-like kinase ALK5 with an IC of 25 nM.50A 83-01 is a potent inhibitor of TGF- type Ireceptor ALK5 kinase, type I nodal receptor ALK4and type I nodal receptor

11、 ALK7, with IC s of 1250nM, 45 nM and 7.5 nM against the transcriptioninduced by ALK5, ALK4 and ALK7, respectively.Purity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98.24%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChe

12、mE/A_83-01_sodium_salt.html A HYPERLINK https:/www.MedChemE/A_83-01_sodium_salt.html HYPERLINK https:/www.MedChemE/A_83-01_sodium_salt.html 83-01 HYPERLINK https:/www.MedChemE/A_83-01_sodium_salt.html HYPERLINK https:/www.MedChemE/A_83-01_sodium_salt.html sodium HYPERLINK https:/www.MedChemE/A_83-01

13、_sodium_salt.html HYPERLINK https:/www.MedChemE/alk2-in-2.html ALK2-IN-2Cat. No.: HY-10432A Cat. No.: HY-112815A 83-01 sodium is a potent inhibitor of TGF-type I receptor ALK5 kinase, ALK4 and ALK7, withIC s of 12 nM, 45 nM and 7.5 nM against the50transcription induced by ALK5, ALK4 and ALK7,respect

14、ively.ALK2-IN-2 is a potent and selective inhibitor ofactivin receptor-like kinase 2 (ALK2) with an ICof 9 nM, and over 700-fold selectivity againstALK3.50Purity: 95.0%Clinical Data: No Development ReportedSize: 10 mg, 50 mgPurity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg,

15、10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/alk2-in-4.html ALK2-IN-4 HYPERLINK https:/www.MedChemE/alk2-in-4.html HYPERLINK https:/www.MedChemE/alk2-in-4-succinate.html ALK2-IN-4 HYPERLINK https:/www.MedChemE/alk2-in-4-succinate.html HYPERLINK https:/www.MedChemE/alk2-in-4-succinate.ht

16、ml succinateCat. No.: HY-136773 Cat. No.: HY-136773AALK2-IN-4 is a potent ALK2 inhibitor extractedfrom patent WO2020086963A1, compound Formula Ifree base.ALK2-IN-4 succinate is a potent ALK2 inhibitorextracted from patent WO2020086963A1, compoundFormula I free base.Purity: 99.86%Clinical Data: No De

17、velopment ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/alk5-in-8.html ALK5-IN-8 HYPERLINK https:/www.MedChemE/alk5-in-8.html HYPERLINK https:/www.MedChemE/alk5-in-9.html ALK5-I

18、N-9Cat. No.: HY-144043 Cat. No.: HY-144437ALK5-IN-8 is a potent inhibitor of TGFRI (ALK5).ALK5-IN-8 Inhibits the phosphorylation of ALK5 onits downstream signaling proteins (Smad2 or Smad3)by blocking the binding of TGFRI to ligands,thereby affecting or blocking TGF- signaling.ALK5-IN-9 (Compound 8h

19、) is a potent and orallyactive inhibitor of TGFRI (ALK5). ALK5-IN-9inhibits ALK5 autophosphorylation and NIH3T3 cellactivity with IC values of 25 nM and 74.6 nM,50respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg

20、, 5 mg HYPERLINK https:/www.MedChemE/az12601011.html AZ12601011 HYPERLINK https:/www.MedChemE/az12601011.html HYPERLINK https:/www.MedChemE/BIBF0775.html BIBF0775Cat. No.: HY-122856 Cat. No.: HY-13783AZ12601011 is an orally active, selective TGFBR1kinase inhibitor with an IC50 of 18 nM and a Kdof 2.

21、9 nM. AZ12601011 inhibits phosphorylation ofSMAD2 via selectively inhibiting ALK4, TGFBR1,and ALK7. AZ12601011 inhibits mammary tumorgrowth .BIBF0775 is a potent and selective transforminggrowth factor (TGF) type I receptor (Alk5)inhibitor with an IC of 34 nM.50Purity: 99.25%Clinical Data: No Develo

22、pment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/bio-013077-01.html BIO-013077-01 HYPERLINK https:/www.Med

23、ChemE/bio-013077-01.html HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html BMP HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html signaling HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html HYPERLINK https:/

24、www.MedChemE/bmp-signaling-agonist-sb4.html agonist HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html HYPERLINK https:/www.MedChemE/bmp-signaling-agonist-sb4.html sb4Cat. No.: HY-118810 Cat. No.: HY-124697BIO-013077-01 is a pyrazole TGF- inhibitor.BMP signaling agonist sb4 is a potent ben

25、zoxazolebone morphogenetic protein 4 (BMP4) signalingagonist with a EC value of 74 nM, activates50BMP signaling by stabilizing intracellularp-SMAD-1/5/9.Purity: 98.16%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 10 mM

26、1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-986260.html BMS-986260 HYPERLINK https:/www.MedChemE/bms-986260.html HYPERLINK https:/www.MedChemE/chromenone-1.html Chromenone HYPERLINK https:/www.MedChemE/chromenone-1.html HYPERLINK https:/www.MedChemE/chromenone-1.html 1Cat. No.: HY-W

27、107024 Cat. No.: HY-143891BMS-986260, an immuno-oncology agent, is a potent,selective, and orally active TGFR1 inhibitor(IC =1.6 nM). BMS-986260 displays exquisite50selectivity for TGFR1 over its isozyme TGFR2, aswell as in a panel of more than 200 kinasesexamined.Chromenone 1 is a potent osteogenic

28、 bonemorphogenetic protein (BMP) potentiator.Chromenone 1 exhibits a unique mode of action asit induces a pronounced, kinase-independent,negative TGF feedback that enhances nuclearBMP-Smad signaling outputs.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No

29、 Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cjj300.html CJJ300 HYPERLINK https:/www.MedChemE/cjj300.html HYPERLINK https:/www.MedChemE/DMH-1.html DMH-1Cat. No.: HY-146693 Cat. No.: HY-12273CJJ300 is a transforming growth factor- (TGF-)inhibitor with an IC of 5.3 M. CJJ300 inh

30、ibits50TGF- signaling by disrupting the formation of theTGF-TR-I-TR-II signaling complex.DMH-1 is a potent and selective BMP inhibitorwith IC s of 27/107.9/98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.81%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100

31、 mg HYPERLINK https:/www.MedChemE/dorsomorphin.html Dorsomorphin HYPERLINK https:/www.MedChemE/dorsomorphin.html HYPERLINK https:/www.MedChemE/Dorsomorphin-dihydrochloride.html Dorsomorphin HYPERLINK https:/www.MedChemE/Dorsomorphin-dihydrochloride.html HYPERLINK https:/www.MedChemE/Dorsomorphin-dih

32、ydrochloride.html dihydrochloride(Compound C; BML-275) Cat. No.: HY-13418A (Compound C dihydrochloride; BML-275 dihydrochloride) Cat. No.: HY-13418Dorsomorphin (Compound C) is a selective andATP-competitive AMPK inhibitor (K=109 nM inithe absence of AMP). Dorsomorphin (BML-275)selectively inhibits B

33、MP type I receptors ALK2,ALK3, and ALK6. Dorsomorphin induces autophagy.Dorsomorphin dihydrochloride (BML-275dihydrochloride; Compound C dihydrochloride) is apotent, selective and ATP-competitive AMPKinhibitor, with a K of 109 nM.iPurity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

34、 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ew-7195.html EW-7195 HYPERLINK https:/www.MedChemE/ew-7195.html HYPERLINK https:/www.MedChemE/fresolimumab.html FresolimumabCat. No.: HY-18766(GC1

35、008) Cat. No.: HY-P99020EW-7195 is a potent and selective ALK5 (TGFR1)inhibitor with an IC of 4.83 nM. EW-7195 has50300-fold selectivity for ALK5 over p38.EW-7195 efficiently inhibits TGF-1-induced Smadsignaling, epithelial-to-mesenchymal transition(EMT) and breast tumour metastasis to the lung.Fres

36、olimumab (GC1008) is a high-affinity fullyhuman monoclonal antibody that neutralizes theactive form of human TGF1, TGF2, and TGF3.Fresolimumab can be used for the research ofcancer and fibrotic diseases .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No De

37、velopment ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/LY2157299.html Galunisertib(LY2157299) Cat. No.: HY-13226 HYPERLINK https:/www.MedChemE/GW788388.html GW788388Cat. No.: HY-10326Galunisertib (LY2157299) is an oral and selectiveTGF- receptor type I (TGF-RI) kinase inhibit

38、orwith an IC of 56 nM.50GW788388 is a potent and selective inhibitor ofALK5 with IC of 18 nM, and also inhibits TGF-50type II receptor and activin type II receptoractivities, without inhibiting BMP type IIreceptor.Purity: 99.95%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity

39、: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/in-1130.html IN-1130 HYPERLINK https:/www.MedChemE/in-1130.html HYPERLINK https:/www.MedChemE/isosaponarin.html IsosaponarinCat. No.: HY-18758 Cat. No.: HY-N2589IN-1130 is a highl

40、y selective transforminggrowth factor- type I receptor kinase (ALK5)inhibitor with an IC of 5.3 nM for ALK5-mediated50Smad3 phosphorylation.Isosaponarin is a flavone glycoside isolated fromwasabi leaves. Isosaponarin increases collagensynthesis, caused by up-regulated TGF- type IIreceptor (TR-II) an

41、d prolyl 4-hydroxylase (P4H)proteins production.Purity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.59%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/ITD-1.html ITD-1 HYPERLINK https:/www.MedChemE/ITD-1.htm

42、l HYPERLINK https:/www.MedChemE/K02288.html K02288Cat. No.: HY-12704 Cat. No.: HY-12278ITD-1 is the first selective TGF receptorinhibitor with an IC of 460 nM.50K02288 is a potent bone morphogenetic protein(BMP) type I receptor inhibitor with IC s of501.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6,respect

43、ively. K02288 shows slightly weakerinhibition against ALK3 and ALK6 with IC s of of505-34 nM.Purity: 99.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChem

44、E/LDN-212854.html LDN-212854 HYPERLINK https:/www.MedChemE/LDN-212854.html HYPERLINK https:/www.MedChemE/LDN-214117.html LDN-214117Cat. No.: HY-15897 Cat. No.: HY-16712LDN-212854 is a novel BMP inhibitor that exhibitssubstantially greater selectivity for BMP versusthe TGF- type I receptors; possesse

45、s a biastowards ALK2(IC50=1.3 nM) versus ALK1 and ALK3compared to other inhibitors.LDN-214117 is a potent and selective ALK2inhibitor with IC50 of 22 nM; 100 foldselectivity for ALK5; also inhibits BMP6(IC50=100nM).Purity: 99.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25

46、 mg, 50 mgPurity: 99.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LDN193189.html LDN193189 HYPERLINK https:/www.MedChemE/LDN193189.html HYPERLINK https:/www.MedChemE/LDN193189-Hydrochloride.html LDN193189 HYPERLINK https:/

47、www.MedChemE/LDN193189-Hydrochloride.html HYPERLINK https:/www.MedChemE/LDN193189-Hydrochloride.html Tetrahydrochloride(DM-3189) Cat. No.: HY-12071Cat. No.: HY-12071ALDN193189 (DM-3189) is a selective BMP type Ireceptor inhibitor, which efficiently inhibitsALK2 and ALK3 (IC =5 nM and 30 nM,50respect

48、ively), with weaker effects on ALK4, ALK5and ALK7 (IC 500 nM).50LDN193189 Tetrahydrochloride is a selective BMPtype I receptor inhibitor, which efficientlyinhibits ALK2 and ALK3 (IC =5 nM and 30 nM,50respectively), with weaker effects on ALK4, ALK5and ALK7 (IC 500 nM).50Purity: 99.48%Clinical Data:

49、No Development ReportedSize: 5 mg, 10 mg, 50 mgPurity: 98.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html LSKL, HYPERLINK https:/www.MedC

50、hemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html Inhibitor HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html of HYPERLINK ht

51、tps:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html Thrombospondin HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.ht

52、ml (TSP-1) HYPERLINK https:/www.MedChemE/LSKL,_Inhibitor_of_Thrombospondin_TSP-1.html HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html LSKL, HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thro

53、mbospondin-tsp-1-tfa.html Inhibitor HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html of HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html HYPERLINK https:/www.MedChe

54、mE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html Thrombospondin HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html (TSP-1) HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-t

55、fa.html HYPERLINK https:/www.MedChemE/lskl-inhibitor-of-thrombospondin-tsp-1-tfa.html (TFA)Cat. No.: HY-P0299 Cat. No.: HY-P0299ALSKL, Inhibitor of Thrombospondin (TSP-1) is alatency-associated protein (LAP)-TGF derivedtetrapeptide and a competitive TGF-1 antagonist.LSKL, Inhibitor of Thrombospondin

56、 (TSP-1) inhibitsthe binding of TSP-1 to LAP and alleviates renalinterstitial fibrosis and hepatic fibrosis.LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is alatency-associated protein (LAP)-TGF derivedtetrapeptide and a competitive TGF-1 antagonist.Purity: 98%Clinical Data: No Development ReportedS

57、ize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 99.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/LY-364947.html LY-364947(HTS466284) Cat. No.: HY-13462 HYPERLINK https:/www.MedChemE/LY2109761.html LY2109761Cat. No.: HY-12075LY-364947 (HTS46628

58、4) is a potent ATP-competitiveinhibitor of TGFR-I with IC of 59 nM, and50exhibits 7-fold selectivity over TGFR-II.LY2109761 is an orally active, selective TGF-receptor type I/II inhibitor with Ks of 38 nM andi300 nM, respectively.Purity: 98.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

59、5 mg, 10 mg, 50 mgPurity: 99.88%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/LY3200882.html LY3200882 HYPERLINK https:/www.MedChemE/LY3200882.html HYPERLINK https:/www.MedChemE/maohuoside-a.html Maohuoside HYPERLINK https:/w

60、ww.MedChemE/maohuoside-a.html HYPERLINK https:/www.MedChemE/maohuoside-a.html ACat. No.: HY-103021 Cat. No.: HY-N4019LY3200882 is a potent, highly selective,ATP-competitive and orally active TGF- receptortype 1 (ALK5) inhibitor with an IC of 38.2 nM.50LY3200882 inhibits various pro-tumorigenicactivi