Dihydroorotate-Dehydrogenase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html Dihydroorotate HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html DehydrogenaseDHODHDihydroorotate dehydrogenase (DHODH) is the fourth

2、 enzyme in the de novo pyrimidine biosynthesis pathway, serving as thecatalyst to oxidize the dihydroorotate to orotic acid in the biosynthesis of uridine monophosphate (UMP). DHODH is a knowntarget for autoimmune diseases as well as an important target for malaria.Based on localization and electron

3、 acceptor, DHODHs have classified into two families: Family 1 members are soluble proteinslocalized to the cytosol, while family 2 members are membrane proteins localized to the inner mitochondrial membrane. Family 1 isfurther subdivided into family 1A and family 1B, which use fumarate and NAD+ (res

4、pectively) as electron acceptors. Family 2DHODH enzymes use respiratory quinones as electron acceptors.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html Dihydroorotate HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html HYPERLINK https:/www.Me

5、dChemE/Targets/dihydroorotate-dehydrogenase.html Dehydrogenase HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html HYPERLINK https:/www.MedChemE/Targets/dihydroorotate-dehydrogenase.html Inhibitors HYPERLINK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.html (E/Z)-Ginkgolic HYPERL

6、INK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.html HYPERLINK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.html acid HYPERLINK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.html HYPERLINK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.html C17:2 HYPERLINK https:/www.MedChemE/e-z-ginkgolic-acid-c17-2.

7、html HYPERLINK https:/www.MedChemE/ag-636.html AG-636Cat. No.: HY-N7961 Cat. No.: HY-137463(E/Z)-Ginkgolic acid C17:2, isolated from Ginkgobiloba, can bind with human dihydroorotatedehydrogenase (DHODH) tightly.AG-636 is a potent, reversible, selective andorally active dihydroorotate dehydrogenase (

8、DHODH)inhibitor with an IC of 17 nM. AG-636 has strong50anticancer effects.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ascochlorin-a.html

9、 Ascochlorin HYPERLINK https:/www.MedChemE/ascochlorin-a.html HYPERLINK https:/www.MedChemE/ascochlorin-a.html A(Acremochlorin A) Cat. No.: HY-139632 HYPERLINK https:/www.MedChemE/BAY-2402234.html BAY-2402234Cat. No.: HY-112645Ascochlorin A is a novel and potent hDHODHinhibitor (K = 3.29 M) for trea

10、tment ofDtriple-negative breast cancer.BAY-2402234 is a selective dihydroorotatedehydrogenase (DHODH) inhibitor for the treatmentof myeloid malignancies.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.95%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 1

11、00 mg HYPERLINK https:/www.MedChemE/brd9185.html BRD9185Cat. No.: HY-120924 HYPERLINK https:/www.MedChemE/Brequinar.html Brequinar(DUP785; NSC 368390) Cat. No.: HY-108325BRD9185 is a Dihydroorotate dehydrogenase (DHODH)inhibitor, with an EC of 16 nM against50multidrug-resistant blood-stage parasites

12、 in vitroand is curative after just three doses in a P.berghei mouse model.Brequinar (DUP785) is a potent inhibitor ofdihydroorotate dehydrogenase (DHODH) with an ICof 5.2 nM for human DHODH. Brequinar haspotent activities against a broad spectrum ofviruses. Brequinar also has an anti-SARS2 activity

13、.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.75%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/chikv-in-2.html CHIKV-IN-2 HYPERLINK https:/www.MedChemE/chikv-in-2.html HYPERLINK https:/www.MedChemE/dhodh-in-1.html DHODH-IN-1Cat. No

14、.: HY-132174 Cat. No.: HY-135282CHIKV-IN-2 is a potent inhibitor againstChikungunya virus (CHIKV), with excellent cellularantiviral activity (EC =270 nM) and improved90liver microsomal stability.DHODH-IN-1 (compound 18d) is a potentDihydroorotate Dehydrogenase (DHODH) inhibitorwith an IC of 25 nM. D

15、HODH-IN-1 is an inhibitor50of pyrimidine biosynthesis pathway.Purity: 98.15%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/dhodh-in-11.html DHODH-IN-11 HYPERLINK

16、https:/www.MedChemE/dhodh-in-11.html HYPERLINK https:/www.MedChemE/dhodh-in-12.html DHODH-IN-12Cat. No.: HY-135675 Cat. No.: HY-135676DHODH-IN-11 (Compound 14b) is a Leflunomidederivative and a weak dihydroorotate dehydrogenase(DHODH) inhibitor with a pK of 5.03.aDHODH-IN-12 (Compound 12b) is a Lefl

17、unomidederivative and a weak dihydroorotate dehydrogenase(DHODH) inhibitor with a pK of 5.07.aPurity: 99.94%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: sales

18、MedChemE HYPERLINK https:/www.MedChemE/dhodh-in-13.html DHODH-IN-13 HYPERLINK https:/www.MedChemE/dhodh-in-13.html HYPERLINK https:/www.MedChemE/dhodh-in-14.html DHODH-IN-14Cat. No.: HY-135677 Cat. No.: HY-135678DHODH-IN-13 (Compound 7a) is a hydroxyfurazananalog of A771726. DHODH-IN-13 is a dihydro

19、orotatedehydrogenase (DHODH) inhibitor with an IC of504.3 M for rat liver DHODH. DHODH-IN-13 can beused for rheumatoid arthritis.DHODH-IN-14 (Compound 7l) is a hydroxyfurazananalog of A771726. DHODH-IN-14 is a dihydroorotatedehydrogenase (DHODH) inhibitor with an IC of500.49 M for rat liver DHODH. D

20、HODH-IN-14 can beused for rheumatoid arthritis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dhodh-in-15.html DHODH-IN-15 HYPERLINK https:/www.MedChemE/dhodh-in-15.html HYPERLINK https:

21、/www.MedChemE/dhodh-in-16.html DHODH-IN-16Cat. No.: HY-135679 Cat. No.: HY-139189DHODH-IN-15 (Compound 7b) is a hydroxyfurazananalog of A771726. DHODH-IN-15 is a dihydroorotatedehydrogenase (DHODH) inhibitor with an IC of5011 M for rat liver DHODH. DHODH-IN-15 can beused for rheumatoid arthritis.DHO

22、DH-IN-16 is a potent dihydroorotatedehydrogenase (DHODH) inhibitor with an IC of500.396 nM for human DHODH.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.88%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/dhodh-

23、in-17.html DHODH-IN-17 HYPERLINK https:/www.MedChemE/dhodh-in-17.html HYPERLINK https:/www.MedChemE/dhodh-in-18.html DHODH-IN-18Cat. No.: HY-128068 Cat. No.: HY-139889DHODH-IN-17, a 2-anilino nicotinic acid, is ahuman DHODH inhibitor (IC =0.40 M). DHODH-IN-1750can be used for theresearch of acute my

24、eloidleukemia (AML).DHODH-IN-18 is a human DHODH inhibitor (IC =500.2 nM).Purity: 99.91%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dhodh-in-19.html DHODH-IN-19 HYPERLINK https:/www.MedC

25、hemE/dhodh-in-19.html HYPERLINK https:/www.MedChemE/dhodh-in-20.html DHODH-IN-20Cat. No.: HY-144169 Cat. No.: HY-144371DHODH-IN-19 is a potent inhibitor of DHODH. DHODHis present in the inner membrane of humanmitochondria and is an iron-containingflavin-dependent enzyme. DHODH-IN-19 inhibitstumor gr

26、owth.DHODH-IN-20 (Compound 133) is a potent inhibitorof DHODH. DHODH is present in the inner membraneof human mitochondria and is an iron-containingflavin-dependent enzyme. DHODH-IN-20 inhibitstumor growth. DHODH-IN-20 has the potential forthe research of acute myelogenous leukemia.Purity: 98%Clinic

27、al Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dhodh-in-3.html DHODH-IN-3 HYPERLINK https:/www.MedChemE/dhodh-in-3.html HYPERLINK https:/www.MedChemE/dhodh-in-4.html DHODH-IN-4Cat. No.: HY-135618 Cat. No

28、.: HY-135619DHODH-IN-3 (compound 3) is a potent inhibitor ofHuman DihydroorotateDehydrogenases (HsDHODH) with an IC value50of 261 nM. DHODH-IN-3 binds to the the ubiquinonebinding cavities in DHODH with a Kapp of 32 nM.iDHODH-IN-4 (compound 17) is a human andPlasmodium falciparum dihydroorotatedehyd

29、rogenase (DHODH) inhibitor, with IC values50of 4 M and 0.18 M for PfDHODH and HsDHODH,respectively. DHODH-IN-4 (compound 17) possessantimalarial activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 H

30、YPERLINK https:/www.MedChemE/dhodh-in-8.html DHODH-IN-8 HYPERLINK https:/www.MedChemE/dhodh-in-8.html HYPERLINK https:/www.MedChemE/DSM265.html DSM265Cat. No.: HY-135666 Cat. No.: HY-100184DHODH-IN-8 (Compound 27) is an inhibitor ofhuman and Plasmodium falciparumdihydroorotate dehydrogenase (DHODH)

31、with IC s50of 0.13 M and 47.4 M, and Ks of 0.016 M andi5.6 M, respectively. DHODH-IN-8 has antimalarialactivity.DSM265 is a long-duration inhibitor of P.falciparum dihydroorotate dehydrogenase(PfDHODH) with an IC of 8.9 nM. DSM265 can also50inhibit the growth of Pf3D7 parasites with anEC of 4.3 nM.5

32、0Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.72%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 250 mg, 500 mg HYPERLINK https:/www.MedChemE/dsm502.html DSM502 HYPERLINK https:/www.MedChemE/dsm502.html HYPERLINK https:/www.MedChemE/dsm705.html DSM705Cat

33、. No.: HY-132170 Cat. No.: HY-132171DSM502 is a pyrrole-based DihydroorotateDehydrogenase (DHODH) inhibitor. DSM502 exhibitsnanomolar potency againsts Plasmodium DHODH andPlasmodium parasites, with no inhibition ofmammalian DHODHs.DSM705 is a pyrrole-based DihydroorotateDehydrogenase (DHODH) inhibit

34、or. DSM705 exhibitsnanomolar potency against Plasmodium DHODH andPlasmodium parasites, with no inhibition ofmammalian DHODHs. DSM705 is a potent antimalarialcompound.Purity: 99.57%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Developme

35、nt ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dsm705-hydrochloride.html DSM705 HYPERLINK https:/www.MedChemE/dsm705-hydrochloride.html HYPERLINK https:/www.MedChemE/dsm705-hydrochloride.html hydrochlorideCat. No.: HY-132171A HYPERLINK https:/www.MedChemE/aslan003.html Farudodstat(ASLAN00

36、3) Cat. No.: HY-129239DSM705 hydrochloride, an orally activeantimalarial compound, is a pyrrole-basedDihydroorotate Dehydrogenase (DHODH)inhibitor.Farudodstat (ASLAN003) is an orally active andpotent Dihydroorotate Dehydrogenase (DHODH)inhibitor with an IC of 35 nM for human DHODH50enzyme. Farudodst

37、at inhibits protein synthesis viaactivation of AP-1 transcription factors.Purity: 99.56%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.95%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/dhodh-in-2.html h

38、DHODH-IN-3 HYPERLINK https:/www.MedChemE/dhodh-in-2.html HYPERLINK https:/www.MedChemE/dhodh-in-5.html hDHODH-IN-4Cat. No.: HY-135570 Cat. No.: HY-128787hDHODH-IN-3 (compound 21d) is a humandihydroorotate dehydrogenase (HsDHODH)inhibits measles virus replication with apMIC value of 8.6.50inhibitor,h

39、DHODH-IN-4 is a potent human dihydroorotatedehydrogenase (DHODH) inhibitor, with a pIC of507.8 for human recombinant DHODH. hDHODH-IN-4inhibits measles virus replication, with apMIC of 8.8.50Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.75

40、%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/dhodh-in-7.html hDHODH-IN-5 HYPERLINK https:/www.MedChemE/dhodh-in-7.html HYPERLINK https:/www.MedChemE/dhodh-in-9.html hDHODH-IN-7Cat. No.: HY-135664 Cat. No.: HY-135667DHODH-IN-7 is a human di

41、hydroorotate dehydrogenase(DHODH) inhibitor, with an IC of 0.91 M.50DHODH-IN-7 induces differentiation in acutemyeloid leukemia.DHODH-IN-9 (Compound 10k) is an azine-bearinganalogue and is a human dihydroorotatedehydrogenase inhibitor. DHODH-IN-9 has antiviraleffect with a pMIC of 7.4.50Purity: 98%C

42、linical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/indoluidin-e.html Indoluidin HYPERLINK https:/www.MedChemE/indoluidin-e.html HYPERLINK https:

43、/www.MedChemE/indoluidin-e.html ECat. No.: HY-139825 HYPERLINK https:/www.MedChemE/laflunimus.html Laflunimus(HR325) Cat. No.: HY-101813Indoluidin E selectively inhibits DHODH andsuppresses cancer cell growth.Laflunimus (HR325) is an immunosuppressive agentand an analogue of the Leflunomide-activeme

44、tabolite A77 1726. Laflunimus is an orallyactive inhibitor of dihydroorotate dehydrogenase(DHODH).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.26%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/leflunomid

45、e.html Leflunomide(HWA486; RS-34821; SU101) Cat. No.: HY-B0083 HYPERLINK https:/www.MedChemE/leflunomide-d4.html Leflunomide-d4Cat. No.: HY-B0083SLeflunomide is a pyrimidine synthesis inhibitor,inhibiting dihydroorotate dehydrogenase (DHODH),and acts as a disease-modifying antirheumaticdrug.Leflunom

46、ide-d4 (HWA486-d4) is the deuteriumlabeled Leflunomide. Leflunomide is a pyrimidinesynthesis inhibitor, inhibiting dihydroorotatedehydrogenase (DHODH), and acts as adisease-modifying antirheumatic drug.Purity: 99.72%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98%Clinical Data:Size

47、: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/ML390.html ML390 HYPERLINK https:/www.MedChemE/ML390.html HYPERLINK https:/www.MedChemE/p1788.html P1788Cat. No.: HY-100688 Cat. No.: HY-146317ML390 is a potent dihydroorotate dehydrogenase(DHODH) inhibitor. ML390 is an inducer of myeloiddifferentiation an

48、d causes myeloid differentiationin murine (ER-HoxA9) and human (U937 and THP1)acute myeloid leukemia (AML) models.P1788 is a dihydroorotate dehydrogenase (DHODH)inhibitor. P1788 induces DNA damage.Purity: 98.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity:

49、 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pfdhodh-in-2.html PfDHODH-IN-2 HYPERLINK https:/www.MedChemE/pfdhodh-in-2.html HYPERLINK https:/www.MedChemE/ptc299.html PTC299Cat. No.: HY-W078844 Cat. No.: HY-124593PfDHODH-IN-2, a dihydrothiophenone derivativ

50、e(Compound 11), is a potent Plasmodiumfalciparum dihydroorotate dehydrogenase(PfDHODH) inhibitor with an IC of 1.11 M.50PfDHODH-IN-2 acts as an antimalarial agent and canbe used for the research of malaria.PTC299 is an orally active inhibitor of VEGFAmRNA translation that selectively inhibits VEGFpr

51、otein synthesis at the post-transcriptionallevel. PTC299 is also a potent inhibitor ofdihydroorotate dehydrogenase (DHODH).Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.52%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg

52、, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/rort-dhodh-in-1.html RORt/DHODH-IN-1 HYPERLINK https:/www.MedChemE/rort-dhodh-in-1.html HYPERLINK https:/www.MedChemE/rort-dhodh-in-2.html RORt/DHODH-IN-2Cat. No.: HY-142843 Cat. No.: HY-142834RORt/DHODH-IN-1 (compound (R)-14d) is a potentand orall

53、y active dual RORt/DHODH inhibitor,with IC s of 0.083 M and 0.172 M, respectively.50RORt/DHODH-IN-1 exhibits remarkable in vivoanti-inflammatory activity.RORt/DHODH-IN-2 (compound 1) is a potent dualRORt/DHODH inhibitor. RORt/DHODH-IN-2 can beused for inflammatory bowel disease (IBD)research.Purity:

54、 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/rort-dhodh-in-3.html RORt/DHODH-IN-3 HYPERLINK https:/www.MedChemE/rort-dhodh-in-3.html HYPERLINK https:/www.MedChemE/Tenovin-1.html Tenovin-1Cat. No.: HY-142847 Cat. No.: HY-13423RORt/DHODH-IN-3 (compound (S)-14d) is a dual