Search Result
Results for "
Bcl-2 proteins
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-10087
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Navitoclax
Maximum Cited Publications
92 Publications Verification
ABT-263
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Bcl-2 Family
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Cancer
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Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
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-
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- HY-10087S
-
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Bcl-2 Family
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Cancer
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Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].
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- HY-13407
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BL 193
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Bcl-2 Family
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Cancer
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Gossypol binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
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- HY-P1527
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Bcl-2 Family
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Others
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Bim BH3 is a biological active peptide. (This Bim peptide belongs to the pro-apoptotic Bcl-2 family of proteins.)
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-
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- HY-161577
-
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Bcl-2 Family
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Cancer
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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-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells .
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- HY-115529
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Bcl-2 Family
Apoptosis
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Cancer
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(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, 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 .
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- HY-10087A1
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ABT-263 dihydrochloride
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Bcl-2 Family
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Cancer
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Navitoclax (ABT-263) dihydrochloride is an orally active Bcl-2 inhibitor that binds to various Bcl-2 family proteins, 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 .
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- HY-160108
-
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Bcl-2 Family
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Others
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Bcl-2-IN-17 is a Bcl2 inhibitor and can be used for the research of diseases associated with Bcl anti-apoptotic protein .
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-
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- HY-W751400
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-
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- HY-161410
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PROTACs
Apoptosis
Bcl-2 Family
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Cancer
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WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker) .
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- HY-P2343
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Apoptosis
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Cancer
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BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
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-
- HY-19551
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ApoG2
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Bcl-2 Family
Apoptosis
Autophagy
Fungal
ROS Kinase
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Infection
Cancer
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Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins 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 .
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- HY-17510
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(±)-Gossypol-acetic acid; BL-193 (acetic acid)
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Bcl-2 Family
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Cancer
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Gossypol acetic acid ((±)-Gossypol-acetic acid) binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
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- HY-153953
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Bcl-2 Family
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Cancer
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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-2 family proteins: 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 .
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-
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- HY-159668
-
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ADC Linker
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Cancer
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DL002 is a ADC linker that can be used to synthesize antibody-drug conjugates containing BCL-2 family protein degraders, and it's used in tumor research .
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- HY-P5327
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Bcl-2 Family
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Others
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r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2 family proteins 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.)
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- HY-N1218
-
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Glycosidase
Bcl-2 Family
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Others
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Stellasterol is a natural product. Stellasterol has high affinity towards Bcl-2 protein (Ki: 118.05 nM). Stellasterol is a weak α-glucosidase inhibitor .
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- HY-50868
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INNO-406; NS-187
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Bcr-Abl
Src
Apoptosis
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Cancer
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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-2 family, and induces apoptosis of Ph + leukemia cells. Bafetinib has antitumor activity .
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- HY-15464D
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(S)-(+)-Gossypol acetic acid
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Bcl-2 Family
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Cancer
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(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
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- HY-163764
-
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Bcl-2 Family
Apoptosis
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Cancer
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Bfl-1-IN-4 (Compound 8) is an inhibitor for Bcl-2 associated protein A1 (Bfl-1) with an IC50 of 16.8 μM .
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- HY-P1889
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Bcl-2 Family
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Inflammation/Immunology
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Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins .
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- HY-P1889A
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Bcl-2 Family
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Inflammation/Immunology
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Bim BH3, Peptide IV TFA is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins .
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- HY-13407R
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Bcl-2 Family
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Cancer
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Gossypol (Standard) is the analytical standard of Gossypol. This product is intended for research and analytical applications. Gossypol binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
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- HY-132307
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Bcl-2 Family
Apoptosis
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Cancer
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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-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent .
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- HY-161415
-
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Ligands for E3 Ligase
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Cancer
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BCL-xL/BCL-2 ligand 1 (compound 72-1) is a BCL-xL and BCL-2 protein ligand. BCL-xL/BCL-2 ligand 1 can be connected to the E3 ligase by a linker to form PROTACs (HY-161410) .
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- HY-161254
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Apoptosis
MDM-2/p53
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Inflammation/Immunology
Cancer
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ATPase-IN-3 (compound 6) is a ATPase inhibitor. ATPase-IN-3 has Gastroprotective effect in ethanol-induced gastric ulcers by contribution of anti-apoptotic (BCL-2) and tumor suppressor (P53) proteins .
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- HY-17510R
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Bcl-2 Family
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Cancer
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Gossypol (acetic acid) (Standard) is the analytical standard of Gossypol (acetic acid). This product is intended for research and analytical applications. Gossypol acetic acid ((±)-Gossypol-acetic acid) binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
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- HY-130604
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DT2216
1 Publications Verification
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Bcl-2 Family
PROTACs
Apoptosis
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Cancer
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DT2216 is a potent and selective BCL-XL (Bcl-2 family 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-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-103243
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TCPOBOP
3 Publications Verification
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Bcl-2 Family
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Cancer
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TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss . TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins .
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- HY-15464
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AT-101; R-(-)-gossypol acetic acid
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Bcl-2 Family
Autophagy
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Cancer
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(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
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- HY-127130
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Bcl-2 Family
Apoptosis
Fungal
Antibiotic
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Infection
Cancer
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Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein .
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- HY-170434
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Bcl-2 Family
Caspase
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Cancer
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Bfl-1-IN-6 (Compound 20) is an orally active inhibitor for Bcl-2 related protein A1 (BFL1) with an IC50 of 19 nM. Bfl-1-IN-6 stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor efficacy in mouse models .
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- HY-10969
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GX15-070 Mesylate
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Bcl-2 Family
Autophagy
Parasite
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Infection
Cancer
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Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins 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 .
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- HY-10969A
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GX15-070
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Bcl-2 Family
Autophagy
Parasite
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Infection
Cancer
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Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins 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 .
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- HY-15464A
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AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid
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Bcl-2 Family
Autophagy
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Cancer
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(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
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- HY-P5325
-
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Bcl-2 Family
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Others
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Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family 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.)
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- HY-P1733
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BMF-Y
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Apoptosis
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Cancer
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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 .
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- HY-170648
-
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Thymidylate Synthase
Apoptosis
PI3K
STAT
Bcl-2 Family
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Cancer
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TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers .
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- HY-162826
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Apoptosis
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Cancer
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Apoptosis inducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer (IC50: 12.8 μM) and can induce early apoptosis in breast cancer cells. Apoptosis inducer 27 can bind to DNA molecules, Bax and Bcl-2 proteins, and induce DNA damage .
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- HY-161659
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Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
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Cancer
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Apoptosis inducer 19 (Compound 7g) is an Apoptosis inducer. Apoptosis inducer 19 elevates expression of pro-apoptotic proteins (Bax and caspase-3) and downregulates anti-apoptotic protein (Bcl-2). Apoptosis inducer 19 upregulates cellular reactive oxygen species (ROS) levels and disrupts mitochondrial membrane potential (MMP). Apoptosis inducer 19 can be used for triple-negative breast cancer (TNBC) research .
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- HY-117136
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HDAC
Caspase
Bcl-2 Family
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Cancer
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AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
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- HY-15191B
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(S)-BI-97C1
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Bcl-2 Family
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Cancer
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(S)-Sabutoclax ((S)-BI-97C1), an optically pure apogossypol derivative, is pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. (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 .
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-
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- HY-160921
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SL65.0155 free base
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5-HT Receptor
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Neurological Disease
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Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .
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- HY-N2416
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities . Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis . Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells .
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-
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- HY-146097
-
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P-glycoprotein
Apoptosis
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Cancer
|
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-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
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- HY-163435
-
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Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
|
Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer agent 201 can be used in cancer research .
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- HY-N0674A
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13-Methylpalmatine chloride
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Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Infection
Cancer
|
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
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-
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- HY-113471A
-
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Apoptosis
Bacterial
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Infection
Cancer
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(S)-(-)-Perillic acid is a terpenoid plant extract with antimicrobial and anticancer activities. (S)-(-)-Perillic acid induces cell apoptosis and cell cycle arrest, and increases the levell of Bax, Bcl2, p21 and caspase-3 proteins. (S)-(-)-Perillic acid can be used for cancer and infection research .
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- HY-N0674
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13-Methylpalmatine
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Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
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Infection
Cancer
|
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
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-
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- HY-146817
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
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- HY-N0674B
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13-Methylpalmatine (hydroxyl)
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Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
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Infection
Inflammation/Immunology
Cancer
|
Dehydrocorydaline (13-Methylpalmatine) hydroxyl is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline hydroxyl elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline hydroxyl shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
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- HY-163527
-
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FGFR
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Cancer
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FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
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- HY-164468
-
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Bcl-2 Family
Apoptosis
Autophagy
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Cancer
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Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087) .
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- HY-127057
-
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Androgen Receptor
CDK
MDM-2/p53
Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
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Lambertianic acid is a bioactive diterpene with anti-allergic, antibacterial and anticancer activities. Lambertianic acid decreases androgen receptor protein levels, cellular and secretory levels of prostate-specific antigen. Lambertianic acid also suppresses cell proliferation by inducing G1 arrest, downregulating CDK4/6 and cyclin D1, activating p53, p21 and p27. Lambertianic acid induces Apoptosis and the expression of related proteins, including cleaved caspase-3/9, c-PARP and BAX, and inhibited BCl-2. Lambertianic acid is promising for research of prostate cancer .
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- HY-162886
-
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JNK
Reactive Oxygen Species
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Cancer
|
BSO-07 is a ROS/JNK activator with significant anticancer effects, having an IC50 value of 24.81 μM against human breast cancer (BC) cells. BSO-07 induces apoptosis (Apoptosis) and paraptosis by activating JNK and increasing ROS levels, including enhancing the expression of apoptosis-associated proteins such as PARP, Bax, phosphorylated p53, ATF4, and CHOP, while decreasing the levels of anti-apoptotic proteins like Bcl-2, Bcl-xL, and Survivin. BSO-07 holds promise for research in the field of breast cancer .
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- HY-N4238
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13-Methylpalmatine nitrate
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Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
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Infection
Cancer
|
Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. . Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
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- HY-149918
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
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- HY-123823
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NCX 4016
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COX
Apoptosis
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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-2 family proteins .
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- HY-N3584
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Chonglou Saponin VII
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Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
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Cancer
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Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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- HY-107738
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Z/E-Guggulsterone
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Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
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Cancer
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Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
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- HY-118119
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PGE synthase
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Cancer
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CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
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- HY-169096
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Microtubule/Tubulin
Apoptosis
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Cancer
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DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
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- HY-168623
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EGFR
Apoptosis
Necroptosis
Bcl-2 Family
Caspase
MDM-2/p53
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Cancer
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EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
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- HY-N3584R
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Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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- HY-13559
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Azaspirane
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Apoptosis
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Cancer
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Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
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- HY-123715
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Others
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Cancer
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Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
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- HY-168739
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Topoisomerase
Reactive Oxygen Species
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
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Cancer
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Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
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- HY-157176
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Bcl-2 Family
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Others
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BAX-IN-1 is a potential, selective inhibitor of Bcl-2-associated X protein (BAX).
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- HY-146095
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
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p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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-
- HY-169412
-
|
MDM-2/p53
CDK
Caspase
Bcl-2 Family
Reactive Oxygen Species
p38 MAPK
ERK
JNK
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Cancer
|
MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
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- HY-B0766
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SY801
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Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
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Infection
Inflammation/Immunology
Cancer
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Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
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- HY-162148
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EGFR
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Cancer
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HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
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- HY-N15136
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|
Apoptosis
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Cancer
|
Isomorellinol is a xanthone with an anticancer potency. Isomorellinol induces apoptosis in cholangiocarcinoma cells. Isomorellinol increases the Bax/Bcl-2 protein expression ratio and decreases survivin protein expression in cholangiocarcinoma cells .
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- HY-143235
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
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Cancer
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-P10614
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Apoptosis
Bcl-2 Family
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Others
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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 .
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- HY-149009
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|
Bcl-2 Family
Apoptosis
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Cancer
|
Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1527
-
|
Bcl-2 Family
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Others
|
Bim BH3 is a biological active peptide. (This Bim peptide belongs to the pro-apoptotic Bcl-2 family of proteins.)
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- HY-P2343
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|
Apoptosis
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Cancer
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BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
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- HY-P1889
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Bcl-2 Family
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Inflammation/Immunology
|
Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins .
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- HY-P5327
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|
Bcl-2 Family
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Others
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r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2 family proteins 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.)
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-
- HY-P1889A
-
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Bcl-2 Family
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Inflammation/Immunology
|
Bim BH3, Peptide IV TFA is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins .
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- HY-P5325
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Bcl-2 Family
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Others
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Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family 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.)
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-
- HY-P1733
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BMF-Y
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Apoptosis
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Cancer
|
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 .
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- HY-P10614
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|
Apoptosis
Bcl-2 Family
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Others
|
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 .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-13407
-
-
-
- HY-17510
-
-
-
- HY-15464
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-
-
- HY-N2416
-
-
-
- HY-N0674A
-
-
-
- HY-N0674
-
-
-
- HY-N0674B
-
-
-
- HY-N1218
-
-
-
- HY-13407R
-
-
-
- HY-17510R
-
-
-
- HY-127057
-
-
-
- HY-N4238
-
-
-
- HY-N3584
-
-
-
- HY-107738
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Z/E-Guggulsterone
|
Triterpenes
Structural Classification
Classification of Application Fields
Terpenoids
Plants
Burseraceae
Disease Research Fields
Commiphora wightii
Cancer
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
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-
-
- HY-N3584R
-
|
Structural Classification
Liliaceae
Source classification
Trillium tschonoskii Maxim.
Plants
Steroids
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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-
-
- HY-N15136
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-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10087S
-
|
Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].
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