Topoisomerase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html TopoisomeraseTopoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due tothe intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the

2、 topology of DNA.Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type Itopoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic featureswith the type II topoisomerases,

3、 and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerasecuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. Thisclass is also split into two subclasses: type IIA and type IIB topoisomerases,

4、which possess similar structure and mechanisms.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html Topoisomerase HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Topo

5、isomerase.html HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html & HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html HYPERLINK https:/www.MedChemE/Targets/Topoisomerase.html Agonists HYPERLINK https:/www.MedChemE/_S_-10-Hydroxycamptothecin.html (S)-10-Hydroxycamptothecin(10-HCPT; 10-Hy

6、droxycamptothecin) Cat. No.: HY-N0095 HYPERLINK https:/www.MedChemE/10-hydroxy-camptothecin-d5.html (S)-10-Hydroxycamptothecin-d5(10-HCPT-d5; 10-Hydroxycamptothecin-d5) Cat. No.: HY-N0095S(S)-10-Hydroxycamptothecin(10-HCPT;10-Hydroxycamptothecin) is a DNAtopoisomerase I inhibitor of isolated from th

7、eChinese plant Camptotheca accuminata.(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is thedeuterium labeled (S)-10-Hydroxycamptothecin.(S)-10-Hydroxycamptothecin (10-HCPT) is a DNAtopoisomerase I inhibitor.Purity: 99.38%Clinical Data: Phase 2Size: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: No D

8、evelopment ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/_plusmn_-10-Hydroxycamptothecin.html ()-10-Hydroxycamptothecin()-10-HCPT) Cat. No.: HY-N0275 HYPERLINK https:/www.MedChemE/racemic-evodiamine.html ()-EvodiamineCat. No.: HY-N0114A()-10-Hydroxycamptothecin is an indole alkaloidthat in

9、hibits the activity of topoisomerase Iand has a broad spectrum of anticancer activity.()-Evodiamine, a quinazolinocarboline alkaloid,is a Top1 inhibitor. Evodiamine exhibitsanti-inflammatory, antiobesity, and antitumoreffects. ()-Evodiamine inhibits the proliferationof a wide variety of tumor cells

10、by inducing theirapoptosis.Purity: 99.44%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 250 mg, 500 mg, 1 g HYPERLINK https:/www.MedChemE/9-Aminocamptothecin.html 9-amino-CPT(9-amino-20(S)-camptothecin) Cat. No.: HY-10

11、0309 HYPERLINK https:/www.MedChemE/9-hydroxyellipticine-hydrochloride.html 9-Hydroxyellipticine HYPERLINK https:/www.MedChemE/9-hydroxyellipticine-hydrochloride.html HYPERLINK https:/www.MedChemE/9-hydroxyellipticine-hydrochloride.html hydrochlorideCat. No.: HY-101775A9-amino-CPT (9-amino-20(S)-camp

12、tothecin) is atopoisomerase I inhibitor with potent anticanceractivity.9-Hydroxyellipticine hydrochloride is a inhibitorof Topo II and RyR. 9-Hydroxyellipticinehydrochloride exhibits antitumor, antioxidant andcatecholamine-releasing activities.Purity: 99.05%Clinical Data: Phase 2Size: 10 mM 1 mL, 2

13、mg, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/9-methoxycamptothecin.html 9-Methoxycamptothecin HYPERLINK https:/www.MedChemE/9-methoxycamptothecin.html HYPERLINK https:/www.MedChemE/Aclacinomycin_A_hydrochloride.html Aclacinomyc

14、in HYPERLINK https:/www.MedChemE/Aclacinomycin_A_hydrochloride.html HYPERLINK https:/www.MedChemE/Aclacinomycin_A_hydrochloride.html A HYPERLINK https:/www.MedChemE/Aclacinomycin_A_hydrochloride.html HYPERLINK https:/www.MedChemE/Aclacinomycin_A_hydrochloride.html hydrochlorideCat. No.: HY-N6011(Acl

15、arubicin hydrochloride) Cat. No.: HY-N2306A9-Methoxycamptothecin (MCPT), isolated fromNothapodytes foetida, has antitumor activitiesthrough topoisomerase inhibition.9-Methoxycamptothecin (MCPT) induces strong G2/Marrest and apoptosis in cancer.Aclacinomycin A hydrochloride (Aclarubicinhydrochloride)

16、, a fluorescent molecule and thefirst described non-peptidic inhibitor showingdiscrete specificity for the CTRL(chymotrypsin-like) activity of the 20Sproteasome.Purity: 99.41%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 95.16%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10

17、 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/INNO-206.html Aldoxorubicin HYPERLINK https:/www.MedChemE/INNO-206.html HYPERLINK https:/www.MedChemE/alternariol.html Alternariol(INNO-206; DOXO-EMCH) Cat. No.: HY-16261Cat. No.: HY-N6714Aldoxorubicin (INNO-206) is an albumin-bindingprodrug of Doxorub

18、icin (DNA topoisomerase IIinhibitor), which is released from albumin underacidic conditions. Aldoxorubicin (INNO-206) haspotent antitumor activities in various cancer celllines and in murine tumor models.Alternariol is a mycotoxin produced by Alternariaspecies. AOH inhibits the catalytic activity of

19、topoisomerase I and topoisomerase II enzymes.Purity: 95.99%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/amonafide.html Amonafide(AS1413

20、) Cat. No.: HY-10982 HYPERLINK https:/www.MedChemE/amonafide-d6.html Amonafide-d6(AS1413-d6) Cat. No.: HY-10982SAmonafide is a topoisomerase II inhibitor andDNA intercalator that induces apoptotic signalingby blocking the binding of Topo II to DNA.Amonafide-d6 (AS1413-d6) is the deuterium labeledAmo

21、nafide. Amonafide is a topoisomerase IIinhibitor and DNA intercalator that inducesapoptotic signaling by blocking the binding ofTopo II to DNA.Purity: 99.92%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK

22、https:/www.MedChemE/amrubicin.html Amrubicin(SM-5887) Cat. No.: HY-B0067 HYPERLINK https:/www.MedChemE/Amsacrine.html Amsacrine(m-AMSA; acridinyl anisidide) Cat. No.: HY-13551Amrubicin (SM-5887) is a DNA topoisomerase IIinhibitor, used for the research of cancer.Amsacrine (m-AMSA; acridinyl anisidid

23、e) is aninhibitor of topoisomerase II, and acts as anantineoplastic agent which can intercalates intothe DNA of tumor cells.Purity: 98.0%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.98%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/amsacrine-

24、hydrochloride.html Amsacrine HYPERLINK https:/www.MedChemE/amsacrine-hydrochloride.html HYPERLINK https:/www.MedChemE/amsacrine-hydrochloride.html hydrochloride(m-AMSA hydrochloride; acridinyl anisidide hydrochloride) Cat. No.: HY-13551A HYPERLINK https:/www.MedChemE/aq4.html AQ4Cat. No.: HY-121649A

25、msacrine hydrochloride (m-AMSA hydrochloride;acridinyl anisidide hydrochloride) is an inhibitorof topoisomerase II, and acts as anantineoplastic agent which can intercalates intothe DNA of tumor cells.AQ4 is a topoisomerase II inhibitor and DNAintercalator as a chemically stable cytotoxicagent in ma

26、ny human tumor lines.Purity: 98.98%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/arn-21934.html ARN-21934 HYPERLINK https:/www.MedChemE/arn-21934.html HYPERLINK https:/www.MedChemE/

27、aurintricarboxylic-acid.html Aurintricarboxylic HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html acidCat. No.: HY-137466 Cat. No.: HY-122575ARN-21934 is a potent, highly selective,blood-brain barrier (BBB) penetrant inhibitor forhu

28、man topoisomerase II over . ARN-21934inhibits DNA relaxation with an IC of 2 M as50compared to the anticancer agent Etoposide(IC =120 M).50Purity: 98.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgAurintricarboxylic acid is a nanomolar-potency,allosteric

29、antagonist with selectivity towards-methylene-ATP-sensitive P2X1Rs and P2X3Rs,with IC s of 8.6 nM and 72.9 nM for rP2X1R and50rP2X3R, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/azd5099.html AZD5099 HYPERLINK https:/www.MedChem

30、E/azd5099.html HYPERLINK https:/www.MedChemE/Banoxantrone_D12.html Banoxantrone HYPERLINK https:/www.MedChemE/Banoxantrone_D12.html HYPERLINK https:/www.MedChemE/Banoxantrone_D12.html (D12)Cat. No.: HY-12888(AQ4N D12) Cat. No.: HY-13562SAZD5099, an antibacterial agent, is a potent andselective bacte

31、rial topoisomerase II inhibitor.AZD5099 potently inhibits the infections caused byGram-positive and fastidious Gram-negativebacteria.Banoxantrone D12 (AQ4N D12) is the deuteriumlabeled banoxantrone. Banoxantrone is a novelbioreductive agent that can be reduced to astable, DNA-affinic compound AQ4, w

32、hich is apotent topoisomerase II inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Banoxantrone_dihydrochloride.html Banoxantrone HYPERLINK https:/www.MedChemE/Banox

33、antrone_dihydrochloride.html HYPERLINK https:/www.MedChemE/Banoxantrone_dihydrochloride.html dihydrochloride(AQ4N dihydrochloride) Cat. No.: HY-13562A HYPERLINK https:/www.MedChemE/Banoxantrone_D12_dihydrochloride.html Banoxantrone-d12 HYPERLINK https:/www.MedChemE/Banoxantrone_D12_dihydrochloride.h

34、tml HYPERLINK https:/www.MedChemE/Banoxantrone_D12_dihydrochloride.html dihydrochloride(AQ4N-d12 dihydrochloride) Cat. No.: HY-13562ASBanoxantrone dihydrochloride is a novelbioreductive agent that can be reduced to astable, DNA-affinic compound AQ4, which is apotent topoisomerase II inhibitor.Banoxa

35、ntrone D12 dihydrochloride (AQ4N D12dihydrochloride) is the deuterium labeledbanoxantrone dihydrochloride. Banoxantrone is anovel bioreductive agent that can be reduced to astable, DNA-affinic compound AQ4, which is apotent topoisomerase II inhibitor.Purity: 99.17%Clinical Data: No Development Repor

36、tedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/becatecarin.html Becatecarin(NSC 655649; BMS 181176; BMY 27557) Cat. No.: HY-13565 HYPERLINK https:/www.MedChemE/Belotecan_hydrochloride.html Beloteca

37、n HYPERLINK https:/www.MedChemE/Belotecan_hydrochloride.html HYPERLINK https:/www.MedChemE/Belotecan_hydrochloride.html hydrochloride(CKD-602) Cat. No.: HY-13566ABecatecarin is a rebeccamycin analog withantitumor effects. Becatecarin intercalates intoDNA and inhibites the catalytic activity oftopois

38、omerases I/II.Belotecan hydrochloride (CKD-602 hydrochloride), aTopoisomerase I inhibitor, is a syntheticcamptothecin derivative.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.82%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/

39、www.MedChemE/belotecan-d7-hydrochloride.html Belotecan-d7 HYPERLINK https:/www.MedChemE/belotecan-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/belotecan-d7-hydrochloride.html hydrochlorideCat. No.: HY-13566AS HYPERLINK https:/www.MedChemE/berberine.html Berberine(Natural Yellow 18) Cat. No.:

40、HY-N0716Belotecan-d7 hydrochloride is the deuteriumlabeled Belotecan hydrochloride. Belotecanhydrochloride (CKD-602 hydrochloride), aTopoisomerase I inhibitor, is a syntheticcamptothecin derivative.Berberine (Natural Yellow 18) is an alkaloidisolated from the Chinese herbal medicineHuanglian, as an

41、antibiotic. Berberine (NaturalYellow 18) induces reactive oxygen species (ROS)generation and inhibits DNA topoisomerase.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/Berberine-chloride.html B

42、erberine HYPERLINK https:/www.MedChemE/Berberine-chloride.html HYPERLINK https:/www.MedChemE/Berberine-chloride.html chloride HYPERLINK https:/www.MedChemE/Berberine-chloride.html HYPERLINK https:/www.MedChemE/Berberine-chloride-hydrate.html Berberine HYPERLINK https:/www.MedChemE/Berberine-chloride

43、-hydrate.html HYPERLINK https:/www.MedChemE/Berberine-chloride-hydrate.html chloride HYPERLINK https:/www.MedChemE/Berberine-chloride-hydrate.html HYPERLINK https:/www.MedChemE/Berberine-chloride-hydrate.html hydrate(Natural Yellow 18 chloride) Cat. No.: HY-18258 (Natural Yellow 18 chloride hydrate)

44、 Cat. No.: HY-17577Berberine chloride is an alkaloid that acts as anantibiotic. Berberine chloride induces reactiveoxygen species (ROS) generation and inhibits DNAtopoisomerase. Antineoplastic properties.Berberine chloride hydrate (Natural Yellow 18chloride hydrate) is an alkaloid that acts as anant

45、ibiotic. Berberine chloride hydrate inducesreactive oxygen species (ROS) generation andinhibits DNA topoisomerase. Antineoplasticproperties.Purity: 99.66%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 1 g, 5 gPurity: 99.84%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 1 g, 5 g HYPERLINK https:/

46、www.MedChemE/berberine-d6-chloride.html Berberine-d6 HYPERLINK https:/www.MedChemE/berberine-d6-chloride.html HYPERLINK https:/www.MedChemE/berberine-d6-chloride.html chloride HYPERLINK https:/www.MedChemE/berberine-d6-chloride.html HYPERLINK https:/www.MedChemE/Betulinic-acid.html Betulinic HYPERLI

47、NK https:/www.MedChemE/Betulinic-acid.html HYPERLINK https:/www.MedChemE/Betulinic-acid.html acid(Natural Yellow 18-d6 chloride) Cat. No.: HY-18258S (Lupatic acid; Betulic acid) Cat. No.: HY-10529Berberine-d6 (Natural Yellow 18-d6) chloride isthe deuterium labeled Berberine chloride.Berberine chlori

48、de is an alkaloid that acts as anantibiotic. Berberine chloride induces reactiveoxygen species (ROS) generation and inhibits DNAtopoisomerase. Antineoplastic properties.Betulinic acid is a natural pentacyclictriterpenoid, acts as a eukaryotictopoisomerase I inhibitor, with an IC of 5 M,50and possess

49、es anti-HIV, anti-malarial,anti-inflammatory and anti-tumor properties.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: Phase 2Size: 10 mM 1 mL, 100 mg, 200 mg, 500 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/

50、Bisantrene.html Bisantrene(CL216942) Cat. No.: HY-100875 HYPERLINK https:/www.MedChemE/Campathecin.html Camptothecin(Campathecin; (S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560Bisantrene is a highly effective antitumor drug,targets eukaryotic type II topoisomerases.Camptothecin (CPT), a kind of alkal

51、oid, is a DNAtopoisomerase I (Topo I) inhibitor with an IC of50679 nM.Purity: 96.35%Clinical Data: Phase 2Size: 10 mg, 25 mg, 50 mgPurity: 99.69%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/camptothecin-20-s-o-propionate.html Camptothecin-20(S)-O-propionate(C

52、amptothecin-20-O-propionate) Cat. No.: HY-114668 HYPERLINK https:/www.MedChemE/camptothecin-d5.html Camptothecin-d5(Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5) Cat. No.: HY-16560SCamptothecin-20(S)-O-propionate (CZ48), theC20-propionate ester of CPT, is a highly effectiveanticancer agent. Campt

53、othecin-20(S)-O-propionate(CZ48) is a topoisomerase- inhibitor.Camptothecin-d5 (Campathecin-d5) is the deuteriumlabeled Camptothecin. Camptothecin (CPT), a kindof alkaloid, is a DNA topoisomerase I (Topo I)inhibitor with an IC of 679 nM.50Purity: 98.43%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 1

54、0 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ch-0793076.html CH-0793076(TP3076) Cat. No.: HY-107096 HYPERLINK https:/www.MedChemE/ch-0793076-tfa.html CH-0793076 HYPERLINK https:/www.MedChemE/ch-0793076-tfa.html HYPERLINK https:/ww

55、w.MedChemE/ch-0793076-tfa.html TFA(TP3076 TFA) Cat. No.: HY-107096BCH-0793076 (TP3076), a hexacyclic camptothecinanalog, is active drug and major metabolite ofTP300. CH-0793076 inhibits DNA topoisomerase Iwith an IC of 2.3 M. CH-0793076 is efficacious50against cells expressing BCRP (breast cancerres

56、istance protein).CH-0793076 (TP3076) TFA, a hexacyclic camptothecinanalog, is active drug and major metabolite ofTP300. CH-0793076 TFA inhibits DNA topoisomerase Iwith an IC of 2.3 M. CH-0793076 TFA is50efficacious against cells expressing BCRP (breastcancer resistance protein).Purity: 98%Clinical D

57、ata: No Development ReportedSize: 1 mg, 5 mgPurity: 98.92%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/chloroquinoxaline-sulfonamide.html Chloroquinoxaline HYPERLINK https:/www.MedChemE/chloroquinoxaline-sulfonamide.html HYPERLINK https:/www.MedChemE/chloroquinoxali

58、ne-sulfonamide.html sulfonamide HYPERLINK https:/www.MedChemE/chloroquinoxaline-sulfonamide.html HYPERLINK https:/www.MedChemE/cl2-mmt-sn38.html CL2-MMT-SN38(Chloroquinoxaline; NSC-339004) Cat. No.: HY-106662Cat. No.: HY-145513Chloroquinoxaline sulfonamide (Chloroquinoxaline),a structural analogue o

59、f sulfaquinoxaline, is atopoisomerase II alpha/beta poison.Chloroquinoxaline sulfonamide is used to controlcoccidiosis in poultry, rabbit, sheep, and cattle.Antitumor activity.CL2-MMT-SN38 is a SN-38 derivative. SN-38, ananticancer agent, is an active metabolite of theTopoisomerase I inhibitor Irino

60、tecan (CPT-11).Purity: 99.47%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/coralyne-chloride.html Coralyne HYPERLINK https:/www.MedChemE/coralyne-chloride.html HYPERLINK https:/www.MedC