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Navitoclax (ABT-263) is a potent and orally active Bcl-2familyprotein inhibitor that binds to multiple anti-apoptotic Bcl-2familyproteins, such as Bcl-xL,Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2familyprotein inhibitor that binds to multiple anti-apoptotic Bcl-2familyproteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
Apogossypolone (ApoG2) is an orally active Bcl-2familyproteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy . Apogossypolone also has antifungal activity .
BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2familyproteins in cancer development and how they impact the survival and proliferation of cancer cells .
(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2proteinfamily, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells .
Navitoclax (Standard) is the analytical standard of Navitoclax. This product is intended for research and analytical applications. Navitoclax (ABT-263) is a potent and orally active Bcl-2familyprotein inhibitor that binds to multiple anti-apoptotic Bcl-2familyproteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
Navitoclax (ABT-263) dihydrochloride is an orally active Bcl-2 inhibitor that binds to various Bcl-2familyproteins, including Bcl-xL, Bcl-2, and Bcl-w, with a Ki value of less than 1 nM. Navitoclax dihydrochloride can be used in cancer research .
Human BAX mRNA encodes the human BCL2 associated X, apoptosis regulator (BAX) protein, a member of the BCL2proteinfamily. BAX forms a heterodimer with BCL2, and functions as an apoptotic activator. It also plays a role in the mitochondrial apoptotic process.
DL002 is a ADC linker that can be used to synthesize antibody-drug conjugates containing BCL-2familyprotein degraders, and it's used in tumor research .
Human BAK1 mRNA encodes the human BCL2 antagonist/killer 1 (BAK1) protein, a member of the BCL2proteinfamily. BAK1 localizes to mitochondria, and functions to induce apoptosis. It also interacts with the tumor suppressor P53 after exposure to cell stress.
Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2family, and induces apoptosis of Ph + leukemia cells. Bafetinib has antitumor activity .
DT2216 is a potent and selective BCL-XL(Bcl-2family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2familyprotein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker) .
r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2familyproteins that constitute a critical control point in apoptosis. r8BIDBH3 is lethal to human leukemia cell lines that expresse Bcl-2. The Bcl-2 antagonists may have the potential to be efficacious in cancer therapy. Poly-D-arginine (d-isomer as denoted by rrrrrrrr) is fused to the Bid BH3 peptide to facilitate cellular uptake of the peptide.)
Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2familyproteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia .
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1)protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent .
Bafetinib (Standard) is the analytical standard of Bafetinib. This product is intended for research and analytical applications. Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity .
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2familyproteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2familyproteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
Triptriolide inhibits Puromycin aminonucleoside PAN (HY-15695)-induced apoptosis in mouse podocytes through regulation of Bcl-2familyproteins and inhibition of Caspase-3. Triptriolide promotes the cell survival, protects and restores the podocyte function through activation of TAK1-NF-κB signaling pathway and upregulation of podocin .
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceaefamily. Solasodine induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2proteins. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities .
Solasodine (Purapuridine) hydrochloride is a steroidal alkaloid that occurs in plants of the Solanaceaefamily. Solasodine hydrochloride induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2proteins. Solasodine hydrochloride has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities .
RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2familyproteinsBcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
(S)-Sabutoclax ((S)-BI-97C1), an optically pure apogossypol derivative, is pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) familyproteins. (S)-Sabutoclax (Compound II) inhibits the binding of BH3 peptides to Bcl-XL, Bcl-2, Mcl-1, and Bfl-1 with IC50 values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. (S)-Sabutoclax also potently inhibits cell growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μM, respectively. (S)-Sabutoclax can be used for the research of apoptosis-based therapies against cancer .
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2familyproteins .
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins(Bcl-2,Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
Bid BH3 peptide is a small peptide derived from Bid protein that can bind and activate the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and apoptosis. Bid BH3 peptide can be used to study mitochondrial bioenergetics .
r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2familyproteins that constitute a critical control point in apoptosis. r8BIDBH3 is lethal to human leukemia cell lines that expresse Bcl-2. The Bcl-2 antagonists may have the potential to be efficacious in cancer therapy. Poly-D-arginine (d-isomer as denoted by rrrrrrrr) is fused to the Bid BH3 peptide to facilitate cellular uptake of the peptide.)
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Bid BH3 peptide is a small peptide derived from Bid protein that can bind and activate the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and apoptosis. Bid BH3 peptide can be used to study mitochondrial bioenergetics .
Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceaefamily. Solasodine induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2proteins. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities .
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins(Bcl-2,Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
Triptriolide inhibits Puromycin aminonucleoside PAN (HY-15695)-induced apoptosis in mouse podocytes through regulation of Bcl-2familyproteins and inhibition of Caspase-3. Triptriolide promotes the cell survival, protects and restores the podocyte function through activation of TAK1-NF-κB signaling pathway and upregulation of podocin .
BAG2 Protein, Human (His) promotes tumorigenesis through enhancing mutant p53 protein levels and function. BAG2 is a target of the c-Myc gene and is involved in cellular senescence via the p21CIP1 pathway.
The BAG-3 protein is a co-chaperone of HSP70 and HSC70, acting as a nucleotide exchange factor to promote the release of ADP from these partners, thus triggering substrate release. BAG-3 Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived BAG-3 protein, expressed by P. pastoris , with N-His labeled tag.
Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2familyprotein inhibitor that binds to multiple anti-apoptotic Bcl-2familyproteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
Human BAX mRNA encodes the human BCL2 associated X, apoptosis regulator (BAX) protein, a member of the BCL2proteinfamily. BAX forms a heterodimer with BCL2, and functions as an apoptotic activator. It also plays a role in the mitochondrial apoptotic process.
Human BAK1 mRNA encodes the human BCL2 antagonist/killer 1 (BAK1) protein, a member of the BCL2proteinfamily. BAK1 localizes to mitochondria, and functions to induce apoptosis. It also interacts with the tumor suppressor P53 after exposure to cell stress.
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