カスパーゼ

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S2228 Belnacasan (VX-765) <1 mg/mL 100 mg/mL 100 mg/mL
S4513 RGD peptide (GRGDNP) 100 mg/mL <1 mg/mL ''<1 mg/mL
S5967 Berberine chloride hydrate 39 mg/mL 78 mg/mL '<1 mg/mL
S6899 Licochalcone D -1 mg/mL 100 mg/mL -1 mg/mL
S3267 Kaempferol-3-O-rutinoside -1 mg/mL 100 mg/mL -1 mg/mL
S6882 HI-TOPK-032 <1 mg/mL 4 mg/mL <1 mg/mL
S8507 Z-YVAD-FMK <1 mg/mL 100 mg/mL <1 mg/mL
S2417 20-Hydroxyecdysone <1 mg/mL 96 mg/mL '96 mg/mL
S7023 Z-VAD-FMK <1 mg/mL 93 mg/mL '''<1 mg/mL
S7314 Z-IETD-FMK <1 mg/mL 91 mg/mL ''<1 mg/mL
S7313 Z-LEHD-FMK TFA 44 mg/mL 100 mg/mL -1 mg/mL
S7312 Z-DEVD-FMK <1 mg/mL 100 mg/mL '<1 mg/mL
S7311 Q-VD-Oph <1 mg/mL 100 mg/mL '100 mg/mL
S8102 Z-VAD(OH)-FMK (Caspase Inhibitor VI) <1 mg/mL 90 mg/mL 90 mg/mL
S7775 Emricasan (IDN-6556) <1 mg/mL 100 mg/mL ''100 mg/mL
S9042 Wedelolactone -1 mg/mL 63 mg/mL -1 mg/mL
S9075 Mulberroside A -1 mg/mL 100 mg/mL -1 mg/mL
S7901 Ac-DEVD-CHO 100 mg/mL -1 mg/mL '-1 mg/mL
S5579 Chelidonic acid -1 mg/mL 4 mg/mL -1 mg/mL
S5584 Citronellol 31 mg/mL <1 mg/mL -1 mg/mL
S1029 Lenalidomide (CC-5013) <1 mg/mL 52 mg/mL <1 mg/mL
S2768 Dinaciclib (SCH727965) <1 mg/mL 26 mg/mL 8 mg/mL
S2738 PAC-1 <1 mg/mL 78 mg/mL 16 mg/mL
S2891 GW441756 <1 mg/mL 25 mg/mL <1 mg/mL
S3224 Cinobufagin -1 mg/mL 100 mg/mL -1 mg/mL
S3238 Resibufogenin -1 mg/mL 100 mg/mL -1 mg/mL
S3275 Senkyunolide I -1 mg/mL 100 mg/mL -1 mg/mL
S0913 4',5,7-Trimethoxyflavone <1 mg/mL 62 mg/mL 15 mg/mL
S9634 Phenoxodiol (Haginin E) <1 mg/mL 48 mg/mL 48 mg/mL
S2927 Apoptosis Activator 2 <1 mg/mL 61 mg/mL <1 mg/mL
S7326 Tasisulam <1 mg/mL 83 mg/mL '83 mg/mL
S6501 NVP 231 <1 mg/mL 86 mg/mL 8 mg/mL
S9276 Alisol B -1 mg/mL 95 mg/mL -1 mg/mL
S2271 Berberine chloride (NSC 646666) <1 mg/mL 40 mg/mL <1 mg/mL
S2448 Gambogic Acid <1 mg/mL 100 mg/mL 100 mg/mL
S0354 Alsterpaullone ' mg/mL
S9097 Alisol B Acetate -1 mg/mL 100 mg/mL -1 mg/mL
S5550 Ethyl gallate -1 mg/mL 39 mg/mL -1 mg/mL
S4353 Terfenadine <1 mg/mL 94 mg/mL '27 mg/mL
S3865 Taurochenodeoxycholic acid -1 mg/mL 99 mg/mL -1 mg/mL
S3088 (±)-Methyl Jasmonate ' mg/mL

亜型選択性的な製品

Caspase製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2228

Belnacasan (VX-765)

Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.

S4513

RGD peptide (GRGDNP)

RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.

S5967

Berberine chloride hydrate

Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6899

Licochalcone D

Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

S3267

Kaempferol-3-O-rutinoside

Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.

S6882

HI-TOPK-032

HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.

S8507

Z-YVAD-FMK

Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.

S2417

20-Hydroxyecdysone

20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.

S7023

Z-VAD-FMK

Z-VAD-FMK (Z-VAD(OH)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

S7314

Z-IETD-FMK

Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor.

S7313

Z-LEHD-FMK TFA

Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a specific, irreversible Caspase-9 inhibitor.

S7312

Z-DEVD-FMK

Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

S7311

Q-VD-Oph

Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.

S8102

Z-VAD(OH)-FMK (Caspase Inhibitor VI)

Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.

S7775

Emricasan (IDN-6556)

Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

S9042

Wedelolactone

Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11.

S9075

Mulberroside A

Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.

S7901

Ac-DEVD-CHO

Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.

S5579

Chelidonic acid

Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.

S5584

Citronellol

Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

S2768

Dinaciclib (SCH727965)

Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.

S2738

PAC-1

PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.

S2891

GW441756

GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.

S3224

Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

S3238

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

S3275

Senkyunolide I

Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.

S0913

4',5,7-Trimethoxyflavone

4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.

S9634

Phenoxodiol (Haginin E)

Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.

S2927

Apoptosis Activator 2

Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.

S7326

Tasisulam

Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

S6501

NVP 231

NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM.

S9276

Alisol B

Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.

S2271

Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S2448

Gambogic Acid

Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.

S0354

Alsterpaullone

Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

S9097

Alisol B Acetate

Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.

S5550

Ethyl gallate

Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity

S4353

Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

S3865

Taurochenodeoxycholic acid

Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.

S3088

(±)-Methyl Jasmonate

(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2228

Belnacasan (VX-765)

Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.

S4513

RGD peptide (GRGDNP)

RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.

S5967

Berberine chloride hydrate

Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6899

Licochalcone D

Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

S3267

Kaempferol-3-O-rutinoside

Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.

S6882

HI-TOPK-032

HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.

S8507

Z-YVAD-FMK

Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.

S2417

20-Hydroxyecdysone

20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.

S7023

Z-VAD-FMK

Z-VAD-FMK (Z-VAD(OH)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

S7314

Z-IETD-FMK

Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor.

S7313

Z-LEHD-FMK TFA

Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a specific, irreversible Caspase-9 inhibitor.

S7312

Z-DEVD-FMK

Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

S7311

Q-VD-Oph

Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.

S8102

Z-VAD(OH)-FMK (Caspase Inhibitor VI)

Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.

S7775

Emricasan (IDN-6556)

Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

S9042

Wedelolactone

Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11.

S9075

Mulberroside A

Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.

S7901

Ac-DEVD-CHO

Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.

S5579

Chelidonic acid

Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.

S5584

Citronellol

Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

2021, 7(6)eabd6263

2021, 118(17)e2023172118

2021, 11(12):5742-5758

S2768

Dinaciclib (SCH727965)

Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.

2021, 7(7)eabd2645

2021, 7(6)eabd6263

2021, 34(11):108870

S2738

PAC-1

PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.

2020, 18;396:122605

2020, 11(6):482

2020, 4;10(5):1585-1597

S2891

GW441756

GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.

2021, 85(3):675-686

2020, canres.1992.2020

2020, 10.1007/s12035-020-02156-1

S3224

Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

S3238

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

S3275

Senkyunolide I

Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.

S0913

4',5,7-Trimethoxyflavone

4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.

S9634

Phenoxodiol (Haginin E)

Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.

S2927

Apoptosis Activator 2

Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.

2021, 13(5):7096-7119

2021, 69(13):3942-3951

2021, 10(2)184

S7326

Tasisulam

Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

2016, 29(6):281-290

S6501

NVP 231

NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM.

S9276

Alisol B

Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.

S2271

Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

2021, 26(5)1210

2021, 10(3)250

2020, 186:105000

S2448

Gambogic Acid

Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.

2019, 10.1158/1078-0432.CCR-19-0775

S0354

Alsterpaullone

Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

S9097

Alisol B Acetate

Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.

S5550

Ethyl gallate

Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity

S4353

Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

S3865

Taurochenodeoxycholic acid

Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.

2019, 7(1):145

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S3088

(±)-Methyl Jasmonate

(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.

Tags: Caspases apoptosis | Caspase inhibition | Caspase activation | Caspase activity | Caspase pathway | Caspase phosphorylation | Caspase cleavage | Caspase activity assay | Procaspase activation | Caspase inhibitor in vivo | Caspase inhibitor clinical trial | Caspase-independent apoptosis | Caspase-dependent apoptosis | Caspase inhibitor review