Caspase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Caspase.html CaspaseCaspase is a family of cysteine proteases that play essential roles in apoptosis (programmed cell death), necrosis, and inflammation.There are two types of apoptotic caspases: initiator (apical) caspases and effector (executioner) caspases.

2、Initiator caspases (e.g.,CASP2, CASP8, CASP9, and CASP10) cleave inactive pro-forms of effector caspases, thereby activating them. Effector caspases (e.g.,CASP3, CASP6, CASP7) in turn cleave other protein substrates within the cell, to trigger the apoptotic process. The initiation of thiscascade rea

3、ction is regulated by caspase inhibitors. CASP4 and CASP5, which are overexpressed in some cases of vitiligo andassociated autoimmune diseases caused by NALP1 variants, are not currently classified as initiator or effector in MeSH, becausethey are inflammatory enzymes that, in concert with CASP1, ar

4、e involved in T-cell maturation.www.MedChemE 12 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Targets/Caspase.html Caspase HYPERLINK https:/www.MedChemE/Targets/Caspase.html HYPERLINK https:/www.MedChemE/Targets/Caspase.html Inhibitors, HYPERLINK https:/www.M

5、edChemE/Targets/Caspase.html HYPERLINK https:/www.MedChemE/Targets/Caspase.html Activators HYPERLINK https:/www.MedChemE/Targets/Caspase.html HYPERLINK https:/www.MedChemE/Targets/Caspase.html & HYPERLINK https:/www.MedChemE/Targets/Caspase.html HYPERLINK https:/www.MedChemE/Targets/Caspase.html Ind

6、ucers HYPERLINK https:/www.MedChemE/15-acetoxyscirpenol.html 15-Acetoxyscirpenol HYPERLINK https:/www.MedChemE/15-acetoxyscirpenol.html HYPERLINK https:/www.MedChemE/2-HBA.html 2-HBACat. No.: HY-N6681 Cat. No.: HY-10366715-acetoxyscirpenol, one of acetoxyscirpenolmoiety mycotoxins (ASMs), strongly i

7、nducesapoptosis and inhibits Jurkat T cell growth in adose-dependent manner by activating othercaspases independent of caspase-3.2-HBA is a potent inducer of NAD(P)H:quinoneacceptor oxidoreductase 1 (NQO1) which can alsoactivate caspase-3 and caspase-10.Purity: 98%Clinical Data: No Development Repor

8、tedSize: 1 mg, 5 mgPurity: 98.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/5-7-dihydroxychromone.html 5,7-Dihydroxychromone HYPERLINK https:/www.MedChemE/5-7-dihydroxychromone.html HYPERLINK https:/www.MedChemE/5-7-4-trime

9、thoxyflavone.html 5,7,4-TrimethoxyflavoneCat. No.: HY-N1970 Cat. No.: HY-N68185,7-Dihydroxychromone, the extract of Cudraniatricuspidata, activates Nrf2/ARE signal and exertsneuroprotective effects against 6-hydroxydopamine(6-OHDA)-induced oxidative stress and apoptosis.5,7,4-Trimethoxyflavone is is

10、olated fromKaempferia parviflora (KP) that is a famousmedicinal plant from Thailand.Purity: 99.98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.78%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/Ac-DEVD-CHO.html Ac-DEVD-CHO HYPERLINK h

11、ttps:/www.MedChemE/Ac-DEVD-CHO.html HYPERLINK https:/www.MedChemE/ac-fltd-cmk.html Ac-FLTD-CMKCat. No.: HY-P1001 Cat. No.: HY-111675Ac-DEVD-CHO is a specific Caspase-3 inhibitorwith a K value of 230 pM.iAc-FLTD-CMK, a gasdermin D (GSDMD)-derivedinhibitor, is a specific inflammatory caspasesinhibitor

12、.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.53%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ac-ietd-afc.html Ac-IETD-AFC HYPERLINK https:/www.MedChemE/ac-ietd-afc.html HYPERLINK https:/www.MedChemE/ac-yvad-cmk.html Ac-YVAD-cmkC

13、at. No.: HY-P1169(Caspase-1 Inhibitor II) Cat. No.: HY-16990Ac-IETD-AFC is a fluorogenic substrate ofcaspase-8, caspase-3, caspase-10, and granzyme B.Ac-YVAD-cmk (Caspase-1 Inhibitor II) is aselective caspase-1 (IL-1beta converting enzyme,ICE) inhibitor with neuroprotective andanti-inflammatory effe

14、cts. Ac-YVAD-cmk effectivelysuppresses the expression of IL-1 and IL-18.Ac-YVAD-cmk inhibits pyroptosis in many diseases.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/akn-028.h

15、tml AKN-028 HYPERLINK https:/www.MedChemE/akn-028.html HYPERLINK https:/www.MedChemE/anticancer-agent-43.html Anticancer HYPERLINK https:/www.MedChemE/anticancer-agent-43.html HYPERLINK https:/www.MedChemE/anticancer-agent-43.html agent HYPERLINK https:/www.MedChemE/anticancer-agent-43.html HYPERLIN

16、K https:/www.MedChemE/anticancer-agent-43.html 43Cat. No.: HY-118304 Cat. No.: HY-146548AKN-028 is an orally active and potent FLT3tyrosine kinase inhibitor (IC = 6nM). AKN-02850causes dose-dependent inhibition of FLT3autophosphorylation.Anticancer Agent 43 is a potent anticancer agent.Anticancer Ag

17、ent 43 induces apoptosis by caspase 3,PARP1, and Bax dependent mechanisms. AnticancerAgent 43 induces DNA damage.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/aristolactam

18、-i.html Aristolactam HYPERLINK https:/www.MedChemE/aristolactam-i.html HYPERLINK https:/www.MedChemE/aristolactam-i.html I(Aristololactam; Aristolactam) Cat. No.: HY-N2013 HYPERLINK https:/www.MedChemE/arnicolide-d.html Arnicolide HYPERLINK https:/www.MedChemE/arnicolide-d.html HYPERLINK https:/www.

19、MedChemE/arnicolide-d.html DCat. No.: HY-N6843Aristololactam I (AL-I), is the main metabolite ofaristolochic acid I (AA-I), participates in theprocesses that lead to renal damage.Arnicolide D is a sesquiterpene lactone isolatedfrom Centipeda minima. Arnicolide D modulatesthe cell cycle, activates th

20、e caspase signalingpathway and inhibits the PI3K/AKT/mTOR andSTAT3 signaling pathways.Purity: 99.69%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/asperosaponin-vi.html Aspero

21、saponin HYPERLINK https:/www.MedChemE/asperosaponin-vi.html HYPERLINK https:/www.MedChemE/asperosaponin-vi.html VICat. No.: HY-N0265 HYPERLINK https:/www.MedChemE/VX-765.html Belnacasan(VX-765) Cat. No.: HY-13205Asperosaponin VI, A saponin component from Dipsacusasper wall, induces osteoblast differ

22、entiationthrough BMP2/p38 and ERK1/2 pathway.Belnacasan (VX-765) is an orally bioactive prodrugof VRT-043198, which is a potent and selectiveinhibitor of IL-converting enzyme (ICE)/caspase-1with Ks of 0.8 nM and less than 0.6 nM foricaspase-1 and caspase-4, respectively.Purity: 98.73%Clinical Data:

23、No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.99%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Biotin-VAD-FMK.html Biotin-VAD-FMKCat. No.: HY-100894 HYPERLINK https:/www.MedChemE/boc-asp-ome-fluoromethyl-ketone.html Boc-Asp(OMe)-f

24、luoromethyl HYPERLINK https:/www.MedChemE/boc-asp-ome-fluoromethyl-ketone.html HYPERLINK https:/www.MedChemE/boc-asp-ome-fluoromethyl-ketone.html ketone(Boc-Asp(OMe)-FMK) Cat. No.: HY-103348Biotin-VAD-FMK is a cell permeable, irreversiblebiotin-labeled caspase inhibitor, used toidentify active caspa

25、ses in cell lysates.Boc-Asp(OME)-Fluoromethyl Ketone is a broad rangecaspase inhibitor that inhibits Fas-mediatedphagocytosis and oxidative rupture inhibition, butdoes not affect the chemotactic activity of IL-8.Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical D

26、ata: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BOC-D-FMK.html BOC-D-FMK HYPERLINK https:/www.MedChemE/BOC-D-FMK.html HYPERLINK https:/www.MedChemE/Chelidonic_acid.html Chelidonic HYPERLINK https:/www.MedChemE/Chelidonic_acid.html HYPERLINK https:/www.MedChemE/Chelidonic_a

27、cid.html acidCat. No.: HY-13229 Cat. No.: HY-W041489Boc-D-FMK is a cell-permeable, irreversible andbroad spectrum caspase inhibitor. Boc-D-FMKinhibits apoptosis stimulated by TNF- with anIC of 39 M.50Chelidonic acid is a component of Chelidoniummajus L., used as an antimicrobial. Chelidonic acidalso

28、 shows anti-inflammatory activity. Chelidonicacid has potential to inhibit IL-6 production byblocking NF-B and caspase-1.Purity: 95.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mgPurity: 95.41%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK

29、 https:/www.MedChemE/crustecdysone.html Crustecdysone HYPERLINK https:/www.MedChemE/crustecdysone.html HYPERLINK https:/www.MedChemE/Dehydrocorydaline.html Dehydrocorydaline(20-Hydroxyecdysone) Cat. No.: HY-N6979 (13-Methylpalmatine) Cat. No.: HY-N0674Crustecdysone (20-Hydroxyecdysone) is a naturall

30、yoccurring ecdysteroid hormone isolated fromCyanotis arachnoides C.B.Clarke which controls theecdysis (moulting) and metamorphosis ofarthropods, it inhibits caspase activity andinduces autophagy via the 20E nuclearDehydrocorydaline (13-Methylpalmatine) is analkaloid that regulates protein expression

31、 ofBax, Bcl-2; activates caspase-7, caspase-8, andinactivates PARP. Dehydrocorydaline elevates p38MAPK activation. Anti-inflammatory andanti-cancer activities.Purity: 99.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.01%Clinical Data: No Development R

32、eportedSize: 10 mM 1 mL, 5 mg, 10 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html Dehydrocorydaline HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html c

33、hloride(13-Methylpalmatine chloride) Cat. No.: HY-N0674A HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html Dehydrocorydaline HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html nitrate(13-Methylpalmatine nitrate) Cat. N

34、o.: HY-N4238Dehydrocorydaline chloride (13-Methylpalmatinechloride) is an alkaloid that regulates proteinexpression of Bax, Bcl-2; activates caspase-7,caspase-8, and inactivates PARP.Dehydrocorydaline chloride elevates p38 MAPKactivation.Dehydrocorydaline nitrate (13-Methylpalmatinenitrate) is an al

35、kaloid. Dehydrocorydalineregulates protein expression of Bax, Bcl-2;activates caspase-7, caspase-8, and inactivatesPARP. Dehydrocorydaline nitrate elevates p38MAPK activation.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.89%Clinical Data: No Development

36、ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/dehydrotrametenolic-acid.html Dehydrotrametenolic HYPERLINK https:/www.MedChemE/dehydrotrametenolic-acid.html HYPERLINK https:/www.MedChemE/dehydrotrametenolic-acid.html acid HYPERLINK https:/www.MedChemE/dehydrotrametenolic-acid.html HYPERLINK

37、 https:/www.MedChemE/destruxin-b.html Destruxin HYPERLINK https:/www.MedChemE/destruxin-b.html HYPERLINK https:/www.MedChemE/destruxin-b.html BCat. No.: HY-N2490 Cat. No.: HY-N6690Dehydrotrametenolic acid is a sterol isolated fromthe sclerotium of Poria cocos. Dehydrotrametenolicacid induces apoptos

38、is through caspase-3 pathway.Dehydrotrametenolic acid has anti-tumor activity,anti-inflammatory, anti-diabetic effects.Destruxin B, isolated from entomopathogenic fungusMetarhizium anisopliae, is one of thecyclodepsipeptides with insecticidal andanticancer activities.Purity: 99.87%Clinical Data: No

39、Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 99.35%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/duocarmycin-a.html Duocarmycin HYPERLINK https:/www.MedChemE/duocarmycin-a.html HYPERLINK https:/www.MedChemE/duocarmycin-a.html A HYPERLINK https:/www.M

40、edChemE/duocarmycin-a.html HYPERLINK https:/www.MedChemE/ef24.html EF24Cat. No.: HY-12455 Cat. No.: HY-119272Duocarmycin A, which is one of well-knownantitumor antibiotics, is a DNA alkylator andefficiently alkylates adenine N3 at the 3 end ofAT-rich sequences in the DNA.EF24 is a curcumin analogue

41、with greateranti-tumor efficacy and oral bioavailability viadeactivation of the MAPK/ERK signaling pathway inoral squamous cell carcinoma (OSCC).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg H

42、YPERLINK https:/www.MedChemE/Emricasan.html Emricasan HYPERLINK https:/www.MedChemE/Emricasan.html HYPERLINK https:/www.MedChemE/EP1013.html EP1013(PF 03491390; IDN-6556) Cat. No.: HY-10396 (F1013) Cat. No.: HY-10397Emricasan (PF 03491390) is an orally active andirreversible pan-caspase inhibitor. E

43、mricasaninhibits Zika virus (ZIKV)-induced increases incaspase-3 activity and protected human corticalneural progenitors.EP1013 (F1013) is a broad-spectrum caspaseselective inhibitor, used in the research of type1 diabetes.Purity: 99.59%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 1

44、0 mg, 50 mg, 100 mgPurity: 97.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Fenbufen.html Fenbufen HYPERLINK https:/www.MedChemE/Fenbufen.html HYPERLINK https:/www.MedChemE/fenbufen-d9.html Fenbufen-d9(CL-82204) Cat. No.: HY-

45、B1138Cat. No.: HY-B1138SFenbufen (CL-82204) is an orally activenon-steroidal anti-inflammatory drug (NSAID), withanalgetic and antipyretic effects. Fenbufen haspotent activity in a variety of animal model,including carageenin edema, UV erythema andadjuvant arthritis.Fenbufen-d9 (CL-82204-d9) is the

46、deuterium labeledFenbufen. Fenbufen (CL-82204) is an orally activenon-steroidal anti-inflammatory drug (NSAID), withantipyretic effects.Purity: 98.99%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgwww.MedChemE 5 HYPERLINK https:/www.M

47、edChemE/Ginsenoside-Rh2.html Ginsenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Rh2.html HYPERLINK https:/www.MedChemE/Ginsenoside-Rh2.html Rh2(20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2) Cat. No.: HY-N0605 HYPERLINK https:/www.MedChemE/gri977143.html GRI977143Cat. No.: HY-100676Ginsenosid

48、e Rh2 induces the activation ofcaspase-8 and caspase-9. Ginsenoside Rh2 inducescancer cell apoptosis in a multi-path manner.GRI977143 is a specific LPA receptor agonist,2with an EC of 3.3 M .50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical Data: N

49、o Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/guggulsterone.html Guggulsterone(Z/E-Guggulsterone) Cat. No.: HY-107738 HYPERLINK https:/www.MedChemE/heptelidic-acid.html Heptelidic HYPERLINK https:/www.MedChemE/heptelidic-acid.html HYPERLINK https:/www.MedChemE/heptelidic-acid.

50、html acid(Koningic acid) Cat. No.: HY-120838Guggulsterone is a plant sterol derived from thegum resin of the tree Commiphora wightii.Heptelidic acid (Koningic acid) is a sesquiterpeneantibiotic. Heptelidic acid inhibitsEtoposide-induced apoptosis via downregulation ofcaspases. Koningic acid (KA) is

51、a specific GAPDHinhibitor with an IC of 90 M.50Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/ivachtin.html Ivachtin(Caspase-3 Inhibitor VII) Cat. No.: HY-P1095

52、HYPERLINK https:/www.MedChemE/kea1-97.html KEA1-97Cat. No.: HY-114982Ivachtin (Caspase-3 Inhibitor VII; compound 7a) isa nonpeptide, noncompetitive and reversiblcaspase-3 inhibitor with an IC of 23 nM.50Ivachtin has modest selectivity for the remainingcaspases.KEA1-97 is a selective Thioredoxin-casp

53、ase 3interaction disruptor (IC =10 M). KEA1-9750disrupts the interaction of thioredoxin withcaspase 3, activates caspases, and inducesapoptosis without affecting thioredoxin activity.Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.66%Clinical Data: No Development ReportedSize

54、: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/lycopodine.html Lycopodine HYPERLINK https:/www.MedChemE/lycopodine.html HYPERLINK https:/www.MedChemE/ML132.html ML132Cat. No.: HY-114372(NCGC 00185682) Cat. No.: HY-12412Lycopodine, a pharmacologically importantbioactive

55、 component derived from Lycopodiumclavatumspores, triggers apoptosis by modulating5-lipoxygenase, and depolarizing mitochondrialmembrane potential in refractory prostate cancercells without modulating p53 activity.ML132 (NCGC 00185682) is a potent and selectivecaspase 1 inhibitor with an IC of 0.316

56、 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/mmpsi.html MMPSI HYPERLINK https:/www.MedChemE/mmpsi.html HYPERLINK https:/www.MedChemE/mpt0b392.html MPT0B392Cat.

57、 No.: HY-103346 Cat. No.: HY-101287MMPSI is a potent and selective small moleculecaspase 3 and caspase 7 inhibitor with an IC50of 1.7 M for human caspase-3.MPT0B392, an orally active quinoline derivative,induces c-Jun N-terminal kinase (JNK) activation,leading to apoptosis.Purity: 98%Clinical Data:

58、No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg6 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/mx1013.html MX1013(CV1013; Z-VD-FMK) Cat. No.: HY-10397A HYPERLINK https:/www.MedChe

59、mE/nivalenol.html NivalenolCat. No.: HY-N6801MX1013 is a potent, irreversible dipeptidecaspase inhibitor vith antiapoptoticactivity. MX1013 inhibits recombinant humancaspase 3 with an IC of 30 nM.50Nivalenol, classified as type B trichotecenestoxins produced by Fusarium graminearum, isa fungal metab

60、olite present in agriculturalproduct. Nivalenol induces cell death throughcaspase-dependent mechanisms and via theintrinsic apoptotic pathway.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedC