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Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
YS-67 is a potent inhibitor of EGFR with an IC 50 of 5.2 nM. YS-67 significantly inhibits p-EGFR and p-AKT. YS-67 inhibits the proliferation of A549, PC-9, and A431cells with IC 50s of 4.1, 0.5, and 2.1 μM, respectively .
PROTAC EGFR degrader 8 (T-184) is a PROTACEGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC .
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.1360, 0.0332, and 0.0339 μM, respectively .
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
PD-L1-IN-1 is a potent PD-L1 inhibitor with an IC50 of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells .
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
EGFR-IN-47 is a potent and orally active EGFR L858R/T790M/C797S inhibitor with an IC50 of 0.01 µM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC .
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
PCSK9 protein, a crucial regulator of plasma cholesterol homeostasis, influences LDL receptor family members like LDLR and VLDLR. It facilitates their degradation within intracellular compartments, enhancing hepatic LDLR degradation through a non-proteolytic mechanism. PCSK9 also exhibits LDLR-independent inhibition of APOB degradation and regulates ENaC-mediated Na(+) absorption, influencing neuronal apoptosis. Notably, it modulates LRP8/APOER2 levels and associated anti-apoptotic pathways. PCSK9 Protein, Human (Biotinylated, HEK293, D374Y, His-Avi) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-Avi, C-His labeled tag and D374Y mutation. The total length of PCSK9 Protein, Human (Biotinylated, HEK293, D374Y, His-Avi) is 662 a.a., with molecular weight of 16 & 66 kDa, respectively.
PCSK9 protein, a crucial regulator of plasma cholesterol homeostasis, influences LDL receptor family members like LDLR and VLDLR. It facilitates their degradation within intracellular compartments, enhancing hepatic LDLR degradation through a non-proteolytic mechanism. PCSK9 also exhibits LDLR-independent inhibition of APOB degradation and regulates ENaC-mediated Na(+) absorption, influencing neuronal apoptosis. Notably, it modulates LRP8/APOER2 levels and associated anti-apoptotic pathways. PCSK9 Protein, Human (D374Y, HEK293, His) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-10*His labeled tag and D374Y mutation. The total length of PCSK9 Protein, Human (D374Y, HEK293, His) is 662 a.a., with molecular weight of ~17 & 70 kDa, respectively.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (HEK293, C-His) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PCSK9 Protein, Human (HEK293, C-His) is 662 a.a., with molecular weight of approximately 20.33 & 59 kDa, respectively.
The PCSK9 protein regulates cholesterol levels by degrading LDLR, VLDLR, LRP1/APOER, and LRP8/APOER2 receptors. It promotes LDLR degradation, inhibits recycling, induces ubiquitination, and affects APOB degradation. Additionally, PCSK9 influences BACE1 intermediates, ENaC surface expression, and neuronal apoptosis by modulating LRP8/APOER2 levels and anti-apoptotic signaling pathways. PCSK9 Protein, Mouse (660a.a, HEK293, His) is the recombinant mouse-derived PCSK9 protein, expressed by HEK293 , with C-His labeled tag. The total length of PCSK9 Protein, Mouse (660a.a, HEK293, His) is 660 a.a., with molecular weight of ~19 & 65 kDa, respectively.
PCSK9 protein, a crucial regulator of plasma cholesterol homeostasis, influences LDL receptor family members like LDLR and VLDLR. It facilitates their degradation within intracellular compartments, enhancing hepatic LDLR degradation through a non-proteolytic mechanism. PCSK9 also exhibits LDLR-independent inhibition of APOB degradation and regulates ENaC-mediated Na(+) absorption, influencing neuronal apoptosis. Notably, it modulates LRP8/APOER2 levels and associated anti-apoptotic pathways. PCSK9 Protein, Human (Biotinylated, V474I, G670E, HEK293, Avi) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-Avi labeled tag and V474I, G670E mutation. The total length of PCSK9 Protein, Human (Biotinylated, V474I, G670E, HEK293, Avi) is 662 a.a., with molecular weight of 19 & 65 kDa, respectively.
PCSK9 protein regulates cholesterol levels by degrading LDLR, VLDLR, LRP1/APOER and LRP8/APOER2 receptors. It promotes LDLR degradation through non-proteolytic mechanisms, disrupts LDLR recycling, induces LDLR ubiquitination, and inhibits APOB degradation. PCSK9 Protein, Rhesus Macaque (HEK293, His) is the recombinant Rhesus Macaque-derived PCSK9 protein, expressed by HEK293 , with C-His labeled tag. The total length of PCSK9 Protein, Rhesus Macaque (HEK293, His) is 662 a.a., with molecular weight of ~20 & 62 kDa, respectively.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (HEK293, Fc) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-mFc labeled tag. The total length of PCSK9 Protein, Human (HEK293, Fc) is 662 a.a., with molecular weight of ~97.4 kDa.
The PCSK9 protein regulates cholesterol levels by interacting with LDLR, VLDLR, LRP1/APOER, and LRP8/APOER2. It promotes their degradation and inhibits their recycling, leading to enhanced LDLR degradation. PCSK9 also affects APOB degradation, BACE1 intermediates, ENaC surface expression, and neuronal apoptosis via LRP8/APOER2. PCSK9 Protein, Rat (HEK293, His) is the recombinant rat-derived PCSK9 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PCSK9 Protein, Rat (HEK293, His) is 661 a.a., with molecular weight of ~17.26 & 60.16 kDa, respectively.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (Biotinylated, V474I, G670E, HEK293, His-HA-Avi) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-Avi, C-HA, C-8*His labeled tag and V474I, G670E, , , mutation. The total length of PCSK9 Protein, Human (Biotinylated, V474I, G670E, HEK293, His-HA-Avi) is 662 a.a., with molecular weight of 18 & 58-70 & 90-150 kDa, respectively.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (HEK293, V474I, G670E, His) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-6*His labeled tag and V474I, G670E, , , mutation. The total length of PCSK9 Protein, Human (HEK293, V474I, G670E, His) is 662 a.a., with molecular weight of 19 & 60 kDa, respectively.
The PCSK9 protein controls plasma cholesterol levels by interacting with LDLR, VLDLR, LRP1/APOER, and LRP8/APOER2 to promote their degradation. It prevents LDLR recycling and directs it to lysosomes for degradation. PCSK9 induces LDLR ubiquitination, inhibits APOB degradation, disposes of BACE1 intermediates, reduces ENaC surface expression, and regulates neuronal apoptosis through LRP8/APOER2. PCSK9 Protein, Macaca nemestrina (HEK293, His) is a recombinant protein dimer complex containing cynomolgus-derived PCSK9 protein, expressed by HEK293, with C-6*His labeled tag. PCSK9 Protein, Macaca nemestrina (HEK293, His), has molecular weight of (16-21) & (55-77) kDa, respectively.
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
