Ras-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Ras.html RasRas is the name given to a family of related proteins which is ubiquitously expressed in all cell lineages and organs. All Ras proteinfamily members belong to a class of protein called small GTPase, and are involved in transmitting signals within ce

2、lls. Ras is theprototypical member of the Ras superfamily of proteins, which are all related in 3D structure and regulate diverse cell behaviours.When Ras is switched on by incoming signals, it subsequently switches on other proteins, which ultimately turn on genes involvedin cell growth, differenti

3、ation and survival. As a result, mutations in ras genes can lead to the production of permanently activatedRas proteins. This can cause unintended and overactive signalling inside the cell, even in the absence of incoming signals. Becausethese signals result in cell growth and division, overactive R

4、as signaling can ultimately lead to cancer. The 3 Ras genes in humans(HRAS,KRAS, and NRAS) are the most common oncogenes in human cancer; Ras inhibitors are being studied as a treatment forcancer, and other diseases with Ras overexpression.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Ras.htm

5、l Ras HYPERLINK https:/www.MedChemE/Targets/Ras.html HYPERLINK https:/www.MedChemE/Targets/Ras.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Ras.html HYPERLINK https:/www.MedChemE/Targets/Ras.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Ras.html HYPERLINK https:/www.MedChemE/Targets

6、/Ras.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Ras.html HYPERLINK https:/www.MedChemE/Targets/Ras.html & HYPERLINK https:/www.MedChemE/Targets/Ras.html HYPERLINK https:/www.MedChemE/Targets/Ras.html Activators HYPERLINK https:/www.MedChemE/minus-rasfonin.html (-)-Rasfonin HYPERLINK http

7、s:/www.MedChemE/minus-rasfonin.html HYPERLINK https:/www.MedChemE/r-ce3f4.html (R)-CE3F4Cat. No.: HY-121532 Cat. No.: HY-108539A(-)-Rasfonin is a fungal secondary metabolite andinhibits small G proteins Ras. (-)-Rasfonininduces apoptosis, necrosis and autophagy in ACHNcells (a renal carcinoma cell l

8、ine).(R)-CE3F4 is a potent and selective inhibitor ofexchange protein directly activated by cAMPisoform 1 (Epac1), with an IC of 4.2 M, with5010-fold selectivity for Epac1 over Epac2 (IC , 4450M). (R)-CE3F4 is more potent than racemic CE3F4and (S)-CE3F4.Purity: 98%Clinical Data: No Development Repor

9、tedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rac-antineoplaston-a10.html (Rac)-Antineoplaston HYPERLINK https:/www.MedChemE/rac-antineoplaston-a10.html HYPERLINK https:/www.MedChemE/rac-antineoplaston-a10.html A10 HYPERLINK https:

10、/www.MedChemE/rac-antineoplaston-a10.html HYPERLINK https:/www.MedChemE/1A-116.html 1A-116Cat. No.: HY-128553A Cat. No.: HY-104064(rac)-Antineoplaston A10 is the racemate ofAntineoplaston A10. Antineoplaston A10 is a Rasinhibitor potentially for the treatment of glioma,lymphoma, astrocytoma and brea

11、st cancer.1A-116 is a Rac1 inhibitor, with antitumoral andantimetastatic effects in several types of cancer,such as breast cancer. 1A-116 preventsRac1-regulated processes involved in the primarytumorigenesis and metastastic processes .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

12、Purity: 99.39%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/6H05.html 6H05 HYPERLINK https:/www.MedChemE/6H05.html HYPERLINK https:/www.MedChemE/6H05-trifluoroacetate.html 6H05 HYPERLINK https:/www.MedChemE/6H05-trifluoroaceta

13、te.html HYPERLINK https:/www.MedChemE/6H05-trifluoroacetate.html (TFA)Cat. No.: HY-12408 Cat. No.: HY-12408A6H05 is a selective, and allosteric inhibitor ofoncogenic mutant K-Ras(G12C). IC50 value: Target:K-Ras G12C 6H05 gives the greatest degree ofmodification, which allosterically modifies theonco

14、genic G12C mutant of highly homologous proteinH-Ras without affecting wild-type K-Ras .6H05 TFA is a selective, and allosteric inhibitorof oncogenic mutant K-Ras(G12C). IC50 value:Target: K-Ras G12C 6H05 gives the greatest degreeof modification, which allosterically modifies theoncogenic G12C mutant

15、 of highly homologous proteinH-Ras without affecting wild-type K-Ras .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/8-cpt-2me-camp-sodium.html 8-CPT-2Me-cAMP HYPERLINK h

16、ttps:/www.MedChemE/8-cpt-2me-camp-sodium.html HYPERLINK https:/www.MedChemE/8-cpt-2me-camp-sodium.html sodium HYPERLINK https:/www.MedChemE/8-cpt-2me-camp-sodium.html HYPERLINK https:/www.MedChemE/mrtx849.html AdagrasibCat. No.: HY-107543(MRTX849) Cat. No.: HY-1301498-CPT-2Me-cAMP sodium is a select

17、ive activator ofexchange proteins activated by cAMP (Epac), thecAMP sensitive guanine nucleotide exchange factors(GEFs) for the small GTPases Rap1 and Rap2.Adagrasib (MRTX849) is a potent, orally-available,and mutation-selective covalent inhibitor of KRASG12C with potential antineoplastic activity.P

18、urity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.85%Clinical Data: Phase 3Size: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/alkannin-1.html Alkannin HYPERLINK https:/www.MedChemE/alkannin-1.html HYPERLINK https:/www.MedChemE/antineoplaston-

19、a10.html Antineoplaston HYPERLINK https:/www.MedChemE/antineoplaston-a10.html HYPERLINK https:/www.MedChemE/antineoplaston-a10.html A10Cat. No.: HY-119874 Cat. No.: HY-128553Alkannin is a potent and specific inhibitor oftumor-specific pyruvate kinase-M2 (PKM2). Alkannindoes not inhibit PKM1 and pyru

20、vate kinase-L (PKL).Alkannin acts as a potential anticancer agent.Antineoplaston A10, a naturally occurringsubstance in human body, is a Ras inhibitorpotentially for the treatment of glioma, lymphoma,astrocytoma and breast cancer.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25

21、 mgPurity: 98.58%Clinical Data: Phase 2Size: 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/aps6-45.html APS6-45 HYPERLINK https:/www.MedChemE/aps6-45.html HYPERLINK https:/www.MedChemE/ARS-1323.html ARS-1323Cat. No.: HY

22、-124944 Cat. No.: HY-U00416APS6-45 is an orally active tumor-calibratedinhibitor (TCI). APS6-45 inhibits RAS/MAPKsignaling and exhibits antitumor activity.ARS-1323, the racemate of ARS-1620, is a novelinhibitor of mutant K-ras G12C extracted frompatent WO 2015054572 A1.Purity: 99.92%Clinical Data: N

23、o Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.14%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/ars-1323-alkyne.html ARS-1323-alkyne HYPERLINK https:/www.MedChemE/ars-1323-alkyne.html HYPERLINK https:/www.MedChemE/AR

24、S-1620.html ARS-1620Cat. No.: HY-128522 Cat. No.: HY-U00418ARS-1323-alkyne, a switch-II pocket (S-IIP)inhibitor, is a conformational specific chemicalreporter of KRASG12C nucleotide state in livingcells.ARS-1620 is an atropisomeric selective KRASG12Cinhibitor with desirable pharmacokinetics.Purity:

25、99.56%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/ARS-1630.html ARS-1630 HYPERLINK https:/www.MedChemE/ARS-1630.html HYPERLIN

26、K https:/www.MedChemE/ARS-853.html ARS-853Cat. No.: HY-U00417 Cat. No.: HY-19706ARS-1630, a less active enantiomer of ARS-1620, isa novel inhibitor of mutant K-ras G12Cextracted from patent WO 2015054572 A1.ARS-853 is a cell-active, selective, covalentKRAS G12C inhibitor with an IC of 2.5 M.50ARS-85

27、3 inhibits mutant KRAS-driven signaling bybinding to the GDP-bound oncoprotein andpreventing activation.Purity: 98.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.39%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 m

28、g, 50 mg HYPERLINK https:/www.MedChemE/asp2453.html ASP2453 HYPERLINK https:/www.MedChemE/asp2453.html HYPERLINK https:/www.MedChemE/atranorin.html AtranorinCat. No.: HY-132966 Cat. No.: HY-N2907ASP2453 is a potent, selective and covalent KRASG12C inhibitor. ASP2453 inhibits the Son ofSevenless (SOS

29、)-mediated interaction between KRASG12C and Raf with an IC value of 40 nM.50Atranorin is a lichen secondary metabolite.Atranorin inhibits lung cancer cell motility andtumorigenesis by affecting AP-1, Wnt, and STATsignaling and suppressing RhoGTPase activity.Purity: 98%Clinical Data: No Development R

30、eportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.41%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/atrovastatin-peg3-fitc.html Atrovastatin-PEG3-FITC HYPERLINK https:/www.MedChemE/atrovastatin-peg3-fitc.html HYPERLINK https:/www.MedChemE/aza1.html AZA1C

31、at. No.: HY-134977(Rac1/Cdc42-IN-1) Cat. No.: HY-136383Atrovastatin-PEG3-FITC (compound S31) is aKRAS-PDE interaction inhibitor.Atrovastatin-PEG3-FITC acts as a ligand influorescence anisotropy assay.AZA1 is a potent dual inhibitor of Rac1 andCdc42. AZA1 induces prostate cancer cellsapoptosis and in

32、hibits prostate cancer cellsproliferation, migration and invasion.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/BAY-293.html BAY-293 HYPERLI

33、NK https:/www.MedChemE/BAY-293.html HYPERLINK https:/www.MedChemE/BDP9066.html BDP9066Cat. No.: HY-114398 Cat. No.: HY-111424BAY-293, a valuable chemical probe, blocks RASactivation via disruption of the KRAS-SOS1interaction with an IC of 21 nM. BAY-293 is a50potent inhibitor of Son of Sevenless 1 (

34、SOS1).SOS1 is the guanine nucleotide exchange factor(GEF) and activator of RAS.BDP9066 is a potent and selective myotonicdystrophy-related Cdc42-binding kinase MRCKinhibitor with an IC of 64 nM for MRCK in SCC1250cells, K values of 0.0136 nM and 0.0233 nM foriMRCK/ in house determinations, respectiv

35、ely.Purity: 98.06%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bi-2852.html BI-2852 HYPERLINK https:/www.MedChemE/bi-2852.html HYPERLINK http

36、s:/www.MedChemE/sos1-in-2.html BI-3406Cat. No.: HY-126247 Cat. No.: HY-125817BI-2852 is a KRAS inhibitor for the switch I/IIpocket (SI/II-pocket) by structure-based drugdesign with nanomolar affinity.BI-3406 (compound I-6) is an orally active, highlypotent and selective inhibitor of the interactionb

37、etween KRAS and Son of Sevenless 1 (SOS1) withan IC of 6 nM. BI-3406 potently reduces the50formation of GTP-loaded KRAS, and inhibits MAPKpathway signaling.Purity: 98.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.79%Clinical Data: No Development Repo

38、rtedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BQU57.html BQU57 HYPERLINK https:/www.MedChemE/BQU57.html HYPERLINK https:/www.MedChemE/CASIN.html CASINCat. No.: HY-12875 Cat. No.: HY-12874BQU57 shows selective inhibition for Ral relativeto Ras or Rho and inhibi

39、t xenograft tumor growthsimilar to depletion of Ral by siRNA. The IC50 forBQU57 of 2.0 M in H2122 and 1.3 M in H358.CASIN is a selective GTPase Cdc42 inhibitor withIC50 of 2 uM.Purity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.82%Clinical Data

40、: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ccg-100602.html CCG-100602 HYPERLINK https:/www.MedChemE/ccg-100602.html HYPERLINK https:/www.MedChemE/CCG-1423.html CCG-1423Cat. No.: HY-120855 Cat. No.: HY-13991CCG-100602 is a specific inhib

41、itor ofmyocardin-related transcription factor A/serumresponse factor (MRTF-A/SRF) signaling.CCG-100602 specifically block MRTF-A nuclearlocalization and thus inhibit the fibrogenictranscription factor SRF.CCG-1423 is a novel inhibitor of RhoA/C-mediatedgene transcription that is capable of inhibitin

42、ginvasion of PC-3 prostate cancer cells in aMatrigel model of metastasis.Purity: 99.66%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/CCG-203971.ht

43、ml CCG-203971 HYPERLINK https:/www.MedChemE/CCG-203971.html HYPERLINK https:/www.MedChemE/ccg-222740.html CCG-222740Cat. No.: HY-108361 Cat. No.: HY-121750CCG-203971 is a second-generation Rho/MRTF/SRFpathway inhibitor. CCG-203971 potently targetsRhoA/C-activated SRE-luciferase (IC =6.4 M).50CCG-203

44、971 inhibits PC-3 cell migration with anIC of 4.2 M. Potential anti-metastasis Agent.50CCG-222740 is an orally active and selectiveRho/myocardin-related transcription factor(MRTF) pathway inhibitor. CCG-222740 is also apotent inhibitor of alpha-smooth muscle actinprotein expression. CCG-222740 effec

45、tively reducesfibrosis in skin and blocks melanoma metastasis.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 E

46、mail: salesMedChemE HYPERLINK https:/www.MedChemE/CID-1067700.html CID-1067700(ML282) Cat. No.: HY-13452 HYPERLINK https:/www.MedChemE/cid44216842.html CID44216842(Cdc42-IN-1) Cat. No.: HY-136379CID-1067700 (ML282) is a pan GTPase inhibitor,and competitively inhibits Ras-related in brain 7(Rab7) wit

47、h a K of 13 nM.iCID44216842 (Cdc42-IN-1) is a potentCdc42-selective guanine nucleotide binding leadinhibitor. The EC s for Cdc42 WT and Cdc42Q61L50mutant are 1.0 and 1.2 M in GTP binding assay,respectively.Purity: 99.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.84

48、%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cmc2-24.html CMC2.24(TRB-N0224) Cat. No.: HY-120793 HYPERLINK https:/www.MedChemE/Deltarasin.html DeltarasinCat. No.: HY-15747CMC2.24 (TRB-N0224), an orally activetricarbonylmethane agent, is

49、 effective againstpancreatic tumor in mice by inhibiting Rasactivation and its downstream effector ERK1/2pathway.Deltarasin is an inhibitor of KRAS-PDEinteraction with K of 38 nM fordbinding to purified PDE.Purity: 96.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50

50、mg, 100 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Deltarasin-hydrochloride.html Deltarasin HYPERLINK https:/www.MedChemE/Deltarasin-hydrochloride.html HYPERLINK https:/www.MedChemE/Deltarasin-hydrochloride.html hy

51、drochlorideCat. No.: HY-15747A HYPERLINK https:/www.MedChemE/diazepinomicin.html Diazepinomicin(ECO-4601; TLN-4601; BU 4664L) Cat. No.: HY-N6674Deltarasin hydrochloride is an inhibitorof KRAS-PDEinteractionwith K of 38 nM for binding todpurified PDE.Diazepinomicin (TLN-4601) is a secondarymetabolite

52、 produced by Micromonospora sp.Diazepinomicin (TLN-4601) inhibits the EGF-inducedRas-ERK MAPK signaling pathway and inducesapoptosis. An anti-tumor agent for K-Ras mutantmodels.Purity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.04%Clinical Data

53、: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Phosphonic_acid,_3E_-1-_2E_-3,7-dimethyl-2,6-octadienyl-4,8-dimethyl-3,7-nonadienylidenebis-,_tetrasodium_salt.html Digeranyl HYPERLINK https:/www.MedChemE/Phosphonic_acid,_3E_-1-_2E_-3,7-dimethyl-2,6-octadienyl-4,8-dimethyl-3,7-nonadienylidene

54、bis-,_tetrasodium_salt.html HYPERLINK https:/www.MedChemE/Phosphonic_acid,_3E_-1-_2E_-3,7-dimethyl-2,6-octadienyl-4,8-dimethyl-3,7-nonadienylidenebis-,_tetrasodium_salt.html bisphosphonate HYPERLINK https:/www.MedChemE/Phosphonic_acid,_3E_-1-_2E_-3,7-dimethyl-2,6-octadienyl-4,8-dimethyl-3,7-nonadien

55、ylidenebis-,_tetrasodium_salt.html HYPERLINK https:/www.MedChemE/EHop-016.html EHop-016(DGBP) Cat. No.: HY-U00145Cat. No.: HY-12810Digeranyl bisphosphonate (DGBP) is a potentgeranylgeranylpyrophosphate (GGPP) synthaseinhibitor, which inhibits geranylgeranylation ofRac1.EHop-016 is a potent and selec

56、tive Rac GTPaseRac1 and Rac3 inhibitor. EHop-016 inhibits Rac1activity with an IC of 1.1 M in MDA-MB-43550cells. EHop-016 inhibits Vav2 interaction withRac, Rac-activated PAK1, lamellipodia formation,and cell migration.Purity: 81.48%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 50 m

57、gPurity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/EHT-1864.html EHT HYPERLINK https:/www.MedChemE/EHT-1864.html HYPERLINK https:/www.MedChemE/EHT-1864.html 1864 HYPERLINK https:/www.MedChemE/EHT-1864.html HYPERLINK https:/www.Me

58、dChemE/EPAC_5376753.html EPAC HYPERLINK https:/www.MedChemE/EPAC_5376753.html HYPERLINK https:/www.MedChemE/EPAC_5376753.html 5376753Cat. No.: HY-16659 Cat. No.: HY-111446EHT 1864 is an inhibitor of Rac family smallGTPases. EHT 1864 directly binds and impairs theability of this small GTPase to engag

59、e criticaldownstream effectors required for growthtransformation.EPAC 5376753 is an allosterically inhibitor ofEpac which inhibits Epac1 with an IC of 4 M in50Swiss 3T3 cells.Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Developm

60、ent ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/esi-08.html ESI-08 HYPERLINK https:/www.MedChemE/esi-08.html HYPERLINK https:/www.MedChemE/FTI-277.html FTI-277Cat. No.: HY-136172 Cat. No.: HY-15872ESI-08 is a potent and selective EPAC antagonist,which can com