Farnesyl-Transferase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html Farnesyl HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html TransferaseFtaseFarnesyl transferase is a zinc-dependent enzyme that catalyzes the attachment of a

2、 farnesyl lipid group to the sulfur atom of acysteine residue of numerous proteins involved in cell signaling including the oncogenic H-Ras protein. Farnesyl transferaseregulates the activation of Ras protein and consequently affects intracellular signal transduction, cell growth and proliferation.F

3、arnesyl transferase is an essential enzyme at downstream of mevalonate (MVA) pathway. Farnesyl transferase catalyzes thefarnesylmoieties of farnesyl pyrophosphate (FPP) coupled to Ras protein, which is dependent on farnesylation anchoring itself inmembrane for its activity. Farnesyl transferase inhi

4、bitors are small-molecule inhibitors that selectively inhibit farnesylation of anumber of intracellular substrate proteins such as Ras. Farnesyl transferase inhibitors represent a new class of agents that targetsignal transduction pathways responsible for the proliferation and survival of diverse ma

5、lignant cell types.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html Farnesyl HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html Transferase HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transf

6、erase.html HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html & HYPERLINK https:/www.MedChemE/Targets/Farnesyl Transferase.html HYPERLINK https:/www

7、.MedChemE/Targets/Farnesyl Transferase.html Antagonists HYPERLINK https:/www.MedChemE/LNK754.html (Rac)-CP-609754(Rac)-LNK-754; (Rac)-OSI-754) Cat. No.: HY-U00401 HYPERLINK https:/www.MedChemE/abt-100.html ABT-100Cat. No.: HY-119257(Rac)-CP-609754 is the racemate of CP-609754.CP-609754 is a farnesyl

8、transferase inhibitor, usedfor the treatment of cancer and Alzheimersdisease.ABT-100 is a potent, highly selective and orallyactive farnesyltransferase inhibitor.Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 98.18%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedCh

9、emE/Arglabin.html Arglabin(+)-Arglabin) Cat. No.: HY-16059 HYPERLINK https:/www.MedChemE/BMS-214662.html BMS-214662Cat. No.: HY-16111Arglabin (+)-Arglabin), a natural productisolated from Artemisia glabella, is a NLRP3inflammasome inhibitor. Arglabin showsanti-inflammatory and antitumor activities.B

10、MS-214662 is a potent and selective farnesyltransferase inhibitor with potent antitumoractivity with an IC of 1.35 nM.50Purity: 99.49%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.59%Clinical Data: Phase 1Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 m

11、g, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cp-609754.html CP-609754(LNK-754; OSI-754) Cat. No.: HY-16373 HYPERLINK https:/www.MedChemE/fgti-2734.html FGTI-2734Cat. No.: HY-128350CP-609754 (LNK-754) is a potent and reversiblefarnesyltransferase inhibitor with potentialanticancer activity.The IC f

12、or inhibiting50farnesylation of recombinant human H-Ras is 0.57ng/mL and recombinant K-Ras is 46 ng/mL.FGTI-2734 is a RAS C-terminal mimetic dual farnesyltransferase (FT) and geranylgeranyl transferase-1(GGT-1) inhibitor with IC s of 250 nM and 520 nM50for FT and GGT-1, respectively.Purity: 99.87%Cl

13、inical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/fgti-2734-mesylate.html FGTI-2734 HYPERLINK https:/www.MedChemE/fgti-2734-mesylate.html HYPERLINK https:/www.MedC

14、hemE/fgti-2734-mesylate.html mesylate HYPERLINK https:/www.MedChemE/fgti-2734-mesylate.html HYPERLINK https:/www.MedChemE/ftase-inhibitor-i.html Ftase HYPERLINK https:/www.MedChemE/ftase-inhibitor-i.html HYPERLINK https:/www.MedChemE/ftase-inhibitor-i.html inhibitor HYPERLINK https:/www.MedChemE/fta

15、se-inhibitor-i.html HYPERLINK https:/www.MedChemE/ftase-inhibitor-i.html ICat. No.: HY-128350A(B581) Cat. No.: HY-128044FGTI-2734 mesylate is a RAS C-terminal mimeticdual farnesyl transferase (FT) and geranylgeranyltransferase-1 (GGT) inhibitor with IC s of 25050nM and 520 nM for FT and GGT, respect

16、ively.Ftase inhibitor I (B581) is a potent, selectiveand peptidomimetic farnesyl transferase (FTase)inhibitor. Ftase inhibitor I shows selectivity forFTase over geranylgeranyl isoprenoid (Ras-GG) orthe fatty acid myristate (Myr-Ras).Purity: 98.73%Clinical Data: No Development ReportedSize: 10 mM 1 m

17、L, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ftase-inhibitor-iii.html Ftase HYPERLINK https:/www.MedChemE/ftase-inhibitor-iii.html HYPERLINK https:/www.MedChemE/ftase-inhibitor-iii.html inhibitor HYPERLINK https:/www.Med

18、ChemE/ftase-inhibitor-iii.html HYPERLINK https:/www.MedChemE/ftase-inhibitor-iii.html III HYPERLINK https:/www.MedChemE/ftase-inhibitor-iii.html HYPERLINK https:/www.MedChemE/FTI_276.html FTI HYPERLINK https:/www.MedChemE/FTI_276.html HYPERLINK https:/www.MedChemE/FTI_276.html 276Cat. No.: HY-142655

19、 Cat. No.: HY-15873Ftase inhibitor III is an anion-dependentFarnesyltransferase inhibitor from a phenotypicscreen.FTI-276 is a protein farnesyl transferase (PFT)inhibitor with IC s of 0.9 and 0.5 nM for50Plasmodium falciparum and human.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 m

20、gPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/fti-276-tfa.html FTI HYPERLINK https:/www.MedChemE/fti-276-tfa.html HYPERLINK https:/www.MedChemE/fti-276-tfa.html 276 HYPERLINK h

21、ttps:/www.MedChemE/fti-276-tfa.html HYPERLINK https:/www.MedChemE/fti-276-tfa.html TFA HYPERLINK https:/www.MedChemE/fti-276-tfa.html HYPERLINK https:/www.MedChemE/fti-2148.html FTI-2148Cat. No.: HY-15873A Cat. No.: HY-118916FTI-276 is a protein farnesyl transferase (PFT)inhibitor with IC s of 0.9 n

22、M and 0.5 nM for50Plasmodium falciparum and human,respectively.FTI-2148 is a RAS C-terminal mimeticdual farnesyl transferase(FT-1) and geranylgeranyl transferase-1(GGT-1) inhibitor with IC s of 1.450nM and 1.7 M, respectively.Purity: 98.06%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg

23、, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fti-2148-ditfa.html FTI-2148 HYPERLINK https:/www.MedChemE/fti-2148-ditfa.html HYPERLINK https:/www.MedChemE/fti-2148-ditfa.html diTFA HYPERLINK https:/www.MedChemE/fti-2148-ditfa.htm

24、l HYPERLINK https:/www.MedChemE/fti-2153.html FTI-2153Cat. No.: HY-118916A Cat. No.: HY-123242FTI-2148 diTFA is a RAS C-terminal mimeticdual farnesyl transferase(FT-1) and geranylgeranyl transferase-1(GGT-1) inhibitor with IC s of 1.450nM and 1.7 M, respectively.FTI-2153 is a potent and highly selec

25、tiveinhibitor of farnesyltransferase (FTase), with anIC of 1.4 nM. FTI-2153 is 3000-fold more50potent at blocking H-Ras (IC , 10 nM) than Rap1A50processing. Anti-cancer activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.41%Clinical Data: No Development ReportedSize:

26、 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/fti-2153-tfa.html FTI-2153 HYPERLINK https:/www.MedChemE/fti-2153-tfa.html HYPERLINK https:/www.MedChemE/fti-2153-tfa.html TFA HYPERLINK https:/www.MedChemE/fti-2153-tfa.html HYPERLINK https:/www.MedChemE/FTI-277.html FTI-2

27、77Cat. No.: HY-123242A Cat. No.: HY-15872FTI-2153 TFA is a potent and highly selectiveinhibitor of farnesyltransferase (FTase), with anIC of 1.4 nM. FTI-2153 TFA is 3000-fold more50potent at blocking H-Ras (IC , 10 nM) than Rap1A50processing. Anti-cancer activity.FTI-277 is an inhibitor of farnesyl

28、transferase(FTase); a highly potent Ras CAAX peptidomimeticwhich antagonizes both H- and K-Ras oncogenicsignaling. FTI-277 can inhibit hepatitis delta virus(HDV) infection.Purity: 98.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data:

29、 No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/FTI-277-hydrochloride.html FTI-277 HYPERLINK https:/www.MedChemE/FTI-277-hydrochloride.html HYPERLINK https:/www.MedChemE/FTI-277-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/FTI-277-hydrochloride.html HYPERLINK

30、 https:/www.MedChemE/L-778123-hydrochloride.html L-778123 HYPERLINK https:/www.MedChemE/L-778123-hydrochloride.html HYPERLINK https:/www.MedChemE/L-778123-hydrochloride.html hydrochlorideCat. No.: HY-15872A(L-778,123 hydrochloride) Cat. No.: HY-16273AFTI-277 hydrochloride is an inhibitor of farnesyl

31、transferase (FTase); a highly potent Ras CAAXpeptidomimetic which antagonizes both H- andK-Ras oncogenic signaling. FTI-277 hydrochloridecan inhibit hepatitis delta virus (HDV) infection.L-778123 hydrochloride is an inhibitor of FPTaseand GGPTase-I with IC50 of 2 nM and 98 nM inenzyme inhibition det

32、ermination.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/lb42708.html LB42708 HYPERLINK https:/www.MedChemE/lb42708.html HYP

33、ERLINK https:/www.MedChemE/Lonafarnib.html LonafarnibCat. No.: HY-15879(Sch66336) Cat. No.: HY-15136LB42708 is a potent, selective and orally activefarnesyltransferase inhibitor. LB42708 inhibitsfarnesylation of H-Ras, N-Ras and K-Ras4B withIC s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.50Lonafarni

34、b (Sch66336) is a potent and orallyactive farnesyl transferase (FTase) inhibitor.Lonafarnib inhibits the activities of H-ras,K-ras and N-ras with IC values of 1.9 nM, 5.250nM and 2.8 nM, respectively. Lonafarnib also hasanti-hepatitis delta virus (HDV) activities.Purity: 98%Clinical Data: No Develop

35、ment ReportedSize: 1 mg, 5 mgPurity: 98.67%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/manumycin-a.html Manumycin HYPERLINK https:/www.MedChemE/manumycin-a.html HYPERLINK https:/www.MedChemE/manumycin-a.html A HYPERLINK https:/www.MedChemE/manumyc

36、in-a.html HYPERLINK https:/www.MedChemE/Benzonitrile,_4-5-4-_3-chlorophenyl_-3-oxo-1-piperazinylmethyl-1H-imidazol-1-ylmethyl-2-phenoxy-.html Prenyl-IN-1Cat. No.: HY-N6796 Cat. No.: HY-U00327Manumycin A is an antibiotic. Manumycin A acts asa selective, competitive inhibitor of proteinfarnesyltransfe

37、rase (FTase) with respect tofarnesylpyrophosphate (K =1.2 M), and as ainoncompetitive inhibitor with respect to the Rasprotein.Prenyl-IN-1 is a protein prenylation inhibitor,especially a geranylgeranyltransferase (GGT) or afarnesyltransferase (FT) inhibitor, exhibitingpotent activity against oxidati

38、ve stress, andparticularly in the treatment of ParkinsonsDisease.Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/RPR107393_free_base.html RPR107393 HYPERLINK https:/www.MedChemE/RPR1073

39、93_free_base.html HYPERLINK https:/www.MedChemE/RPR107393_free_base.html free HYPERLINK https:/www.MedChemE/RPR107393_free_base.html HYPERLINK https:/www.MedChemE/RPR107393_free_base.html base HYPERLINK https:/www.MedChemE/RPR107393_free_base.html HYPERLINK https:/www.MedChemE/tectol.html TectolCat.

40、 No.: HY-100299 Cat. No.: HY-N7634RPR107393 free base is a selective squalenesynthase inhibitor, which inhibits rat livermicrosomal squalene synthase with an IC of 0.850nM.Tectol, isolated from Lippia sidoides, exhibitssignificant activity against human leukemia celllines HL60 and CEM. Tectol is a f

41、arnesyltransferase(FTase) inhibitor with IC s of 2.09 and 1.73 M50for human and T. brucei FTase, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/Tipifarnib.html Tipifarnib(IND 5835

42、9; R115777) Cat. No.: HY-10502 HYPERLINK https:/www.MedChemE/Tipifarnib-S-enantiomer.html Tipifarnib HYPERLINK https:/www.MedChemE/Tipifarnib-S-enantiomer.html HYPERLINK https:/www.MedChemE/Tipifarnib-S-enantiomer.html (S HYPERLINK https:/www.MedChemE/Tipifarnib-S-enantiomer.html HYPERLINK https:/ww

43、w.MedChemE/Tipifarnib-S-enantiomer.html enantiomer)(IND-58359 S enantiomer; (S)-(-)-R-115777) Cat. No.: HY-10502ATipifarnib (IND 58359) binds to and inhibitsfarnesyltransferase (FTase) with an IC of 0.8650nM. Antineoplastic activity.Tipifarnib S enantiomer is the S-enantiomer ofTipifarnib. Tipifarni

44、b is a potent and specificfarnesyltransferase (FTase) inhibitor with IC of500.6 nM. Tipifarnib S enantiomer is the less activeisomer.Purity: 99.89%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 m

45、g HYPERLINK https:/www.MedChemE/ym-53601.html YM-53601 HYPERLINK https:/www.MedChemE/ym-53601.html HYPERLINK https:/www.MedChemE/YM-53601_free_base.html YM-53601 HYPERLINK https:/www.MedChemE/YM-53601_free_base.html HYPERLINK https:/www.MedChemE/YM-53601_free_base.html free HYPERLINK https:/www.MedChemE/YM-53601_free_base.html HYPERLINK https:/www.MedChemE/YM-53601_free_base.html baseCat. No.: HY-100313A Cat. No.: HY-100313YM-53601, a squalene synthase inhibitor, reducesplasma cholesterol and triglyceride levels invivo. YM-53601 inhibits squalene synthase derivedfrom human hepat