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Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC50 values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer .
2-PPA is a lysosomal potassium and proton channel TMEM175 pore blocker. 2-PPA binds at a TMEM175 pore site to occlude potassium and proton ion permeation pathways. 2-PPA increases lysosomal macromolecule catabolism, accelerates macropinocytosis. 2-PPA binds to hepatic protein in covalent. 2-PPA can be used for the research of Parkinson's disease .
MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a Ki of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
SOP1812 (QN-302) is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer .
MASTL-IN-2 is an MASTL (microtubule-associated serine/threonine kinase-like) inhibitor. MASTL-IN-2 inhibits human epithelial MIA PaCa cancer cell proliferation with IC50 of 2.8 nM .
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
Transketolase-IN-4 is a potent inhibitor of transketolase with an IC50 value of 3.9 μM. Transketolase-IN-4 inhibits the proliferation of tumor cells including SW620, LS174T and MIA PaCa-2. Transketolase-IN-4 can be used for tumor research .
DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer .
Tomentosin is an orally active natural sesquiterpenoid lactone. Tomentosin exhibits multiple activities such as anti-tumor, anti-fungal, anti-inflammatory, anti-oxidant and neuroprotective effects. Tomentosin can inhibit tumor cell proliferation, migration and invasion, and induce apoptosis. Tomentosin can be used in the research of tumors, inflammation and nervous system diseases .
BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase .
RM-018 is a potent, functionally distinct tricomplex KRAS G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS G12C .
ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .
Mecbotamab vedotin (BA3011) is a pH dependent antibody drug conjugate (ADC) targeting AXL. Mecbotamab vedotin can significantly inhibit AXL in DU145 cells and LCLC-103H cells and kills cells. Mecbotamab vedotin can be used for research on cancer such as lung cancer, pancreatic cancer and prostate cancer. The antibody component is Mecbotamab (HY-P9988), and the ADC toxin molecule is Monomethyl auristatin E (MMAE) (HY-15162) .
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines .
Akt1-IN-1 (compound 5b) is a potent and selective Akt1 inhibitor with an IC50 value of 18.79 nM in MIA Paca-2 cells. Akt1-IN-1 does not exhibit obvious teratogenicity, hepatotoxicity and cardiotoxicity (No Observed Adverse Effect Level > 100 µM). Akt1-IN-1 can be used for researching anticancer .
ATR-IN-32 is an orally active ATR inhibitor. ATR-IN-32 potently inhibits the proliferation of MIA PaCa-2 cells. ATR-IN-32 exerts significant tumor growth inhibition in mice bearing LOVO and HT-29 xenografts. ATR-IN-32 can be used for the study of cancers mediated by ATR protein kinase, such as colorectal cancer, pancreatic cancer .
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
Nek2-IN-4 is a potent NEK2 inhibitor with an IC50 value of 15 nM. Nek2-IN-4 inhibits cell proliferation. Nek2-IN-4 has the potential for the research of pancreatic cancer .
MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers .
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
ZG-2492 is an orally active LDHA inhibitor with an IC50 of 156 nM. ZG-2492 can reduce lactate production and induce cell cycle arrest and apoptosis in pancreatic cancer cells . ZG-2492 has antitumor activity and can be used in the research of tumors such as pancreatic cancer .
RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research .
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors .
MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
AB19 is a potent Vav1 inhibitor. AB19 inhibits Vav1 and reduces its downstream ERK phosphorylation. AB19 shows anti-proliferative activity in pancreatic cancer models. AB19 can be used for pancreatic cancer research .
Foryshiyanine A is a triterpenoid alkaloid. Foryshiyanine A possesses anti-inflammatory activity, inhibiting the release of β-glucuronidase from rat polymorphonuclear leukocytes. Foryshiyanine A exhibits antiviral activity, with an EC50 of 4.5 μM against respiratory syncytial virus (RSV) and an IC50 of 7.3 μM against influenza A virus (H1N1). Foryshiyanine A reduces viral load by disrupting viral replication and entry. Foryshiyanine A may be used for the researches of inflammation and infection .
MIA Human Pre-designed siRNA Set A contains three designed siRNAs for MIA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mia gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
MIA2 Human Pre-designed siRNA Set A contains three designed siRNAs for MIA2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
MIA3 Human Pre-designed siRNA Set A contains three designed siRNAs for MIA3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mia2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells .
SHP2-IN-22 is SHP2 allosteric inhibitor with an IC50 value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research .
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers .
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers .
KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers .
H2S probe 1 (compound 1NND) is a derivative of nitrobenzoxadiazole (NBD) with antitumor activity. H2S probe 1 is cytotoxic to human pancreatic cancer cell MIA PaCa-2 (IC50=77.9 nM) and has a high affinity for human telomeric G-quadruplex (G4) (Kd=1.72 μM). H2S probe 1 can be used in cancer research .
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers .
JR5-26B is an orally active apoptosis inducer. JR5-26B induces cell death through copper-mediated apoptosis and necroptosis. JR5-26B exhibits antiproliferative activity on MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells with IC50s of 0.6, 4.4, 8.0, 1.1, and 3.4μM, respectively .
EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein KRASG12C with an IC50 of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC50 of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC50 of 3.15 nM and 2.33 nM .
OXPHOS-IN-1 (compound 2) is a oxidative phosphorylation (OXPHOS) inhibitor. OXPHOS-IN-1 inhibits the cells growth of MIA PaCa-2 and BxPC-3 cells with IC50s of 2.34 μM and 13.82 μM, respectively .
KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers .
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
Toyaburgine is a unique isoquinoline compound that exhibits anti-tumor activity. It packs a punch by disrupting the PI3K/AKT/mTOR signaling pathway, causing significant morphological changes and cell death in MIA PaCa-2 cells. On top of that, it puts the brakes on cell migration and colony formation. This compound is showing a lot of promise in the realm of pancreatic cancer research .
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
EGFR-IN-105 (Compound 5b) is an EGFR2 inhibitor with an IC50 value of 0.68 μM. EGFR-IN-105 exhibits anticancer activity and can induce apoptosis in cancer cells, which is used in the research of pancreatic cancer .
FLQY2 is a camptothecin analog that exhibits outstanding antitumor efficacy against various solid tumors. FLQY2 possesses both in vitro and in vivo anti-pancreatic cancer activity, inhibiting cell proliferation, colony formation, inducing apoptosis, and causing cell cycle arrest at nanomolar concentrations .
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis .
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity .
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
hGAPDH-IN-1, a 3-bromo-4,5-dihydroisoxazole derivative, is a specific and potent hGAPDH covalent inhibitor. hGAPDH-IN-1 reduces cancer cell growth in different pancreatic cancer cell lines.
CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 of 1.71 μM. CD13-IN-1 can inhibit the proliferation of multiple tumor cells and has anti-tumor activity .
Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2 .
Mia Rat Pre-designed siRNA Set A contains three designed siRNAs for Mia gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Mia2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Otor Mouse Pre-designed siRNA Set A contains three designed siRNAs for Otor gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
CHK1-IN-15 (compound 9a) is a ATP-kompetitive inhibitor of Checkpoint-Kinase-1 (CHK1) with a 95% binding at 1.0 µM. CHK1-IN-15 is a Chk1 target protein ligand of MA203 (HY-179157). CHK1-IN-15 can be used in cancer-related research .
E3 Ligase Ligand-linker Conjugate 173 is an E3 Ligase Ligand-Linker Conjugate. E3 Ligase Ligand-linker Conjugate 173 can be used to synthesize YN14-H (HY-173250) to induce apoptosis and inhibits migration, and exert antitumor activity in vivo .
PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50 = 4.65 nM) degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability, with EC50 values after 72 h of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines.PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer .
QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model .
POLRMT-IN-3 is a photosensitive inhibitor of mitochondrial RNA polymerase (POLRMT). POLRMT-IN-3 is biologically inactive in the dark but rapidly releases the active parent compound LJ03 upon illumination with 405 nm light, enabling spatiotemporally precise inhibition of POLRMT. POLRMT-IN-3 exhibits antitumor activity and can be used in research on tumors such as pancreatic cancer and ovarian cancer .
2A3 (2-aminopyridine-3-carboxylic acid imidazolide) is a T cell activator that specifically binds to CEACAM6 and CEACAM5. 2A3 exhibits enzymatic activity that catalyzes the glucuronidation of specific substrates (e.g., 1-naphthol), and possesses significant cytotoxic activity. When integrated into CAR T cells or used alone, 2A3 acts by inducing cytokine release, degranulation, and direct cytotoxicity. 2A3 kills pancreatic and breast cancer cells with high target antigen expression in vitro, and significantly inhibits the growth of pancreatic cancer xenografts in vivo. 2A3 broadly targets malignant tumors with overexpressed CEACAM5, CEACAM6, or co-expressed both, and shows high expression mainly in tissues such as the liver and colon. 2A3 serves as an important research tool for the immunotherapy of pancreatic and breast cancer . 2A3 is a novel SHAPE reagent, which can be used for the analysis of RNA structure both in vitro and in vivo . 2A3 is an electrophilic chemical probe that acylates the 2'-OH in the RNA backbone. 2A3 can be used for RNA SHAPE-MaP experiments and is capable of analyzing the RNA secondary structures at single nucleotide resolution.
GPX4-IN-9 (Compound A16) is a glutathione peroxidase 4 (GPX4) inhibitor that specifically targets GPX4 under both in vitro and in vivo conditions, inducing ferroptosis. GPX4-IN-9 exhibits cytotoxicity against pancreatic cancer cells and can be used in cancer research .
SHP2-IN-46 is an orally active SHP2 inhibitor (IC50 = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma .
YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356).
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth .
ADAMTS-4/5-IN-1 is an orally active, and selective dual ADAMTS-4/5 inhibitor with IC50 values of 2 nM for human ADAMTS-4 and human ADAMTS-5, respectively. ADAMTS-4/5-IN-1 exhibits high selectivity against MMP enzymes. ADAMTS-4/5-IN-1 reduces aggrecan degradation products in synovial fluid. ADAMTS-4/5-IN-1 can be used for the research of osteoarthritis .
MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer .
LC-1028 (Compound 20) is an irreversible, non-competitive, covalent p97 inhibitor with a Ki app value of 33.2 nM. LC-1028 covalently modifies the cysteine residues (Cys105, Cys522, Cys535) of p97. LC-1028 can be used in the research of pancreatic cancer .
ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer .
NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model .
MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma .
KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
Geranic acid (Geranate) acts as a tyrosinase inhibitor and antifungal agent, with an IC50 value of 0.14-2.3 mM against mushroom tyrosinase. Geranic acid reduces the viability of human pancreatic cancer cells and B-lymphoma cells. Geranic acid inhibits mycelial growth of the maize pathogens Colletotrichum graminicola and Fusarium graminearum. Geranic acid is applicable to research related to fungal infections, pancreatic cancer and B-lymphoma .
JWJ-01-306 is a CRBN-recruiting ZBTB11Molecular Glues degrader. JWJ-01-306 degrades ZBTB11 and reprograms cellular metabolism, thereby reducing the level of Oxidative Phosphorylation and the activity of the tricarboxylic acid cycle. JWJ-01-306 enhances the response of organoids to K-Ras inhibition. JWJ-01-306 inhibits the proliferation of pancreatic ductal adenocarcinoma cells and melanoma cells. JWJ-01-306 can be used in studies related to pancreatic ductal adenocarcinoma and melanoma .
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
Cys-HW12 is a random peptide containing an N-terminal cysteine. Cys-HW12 can be coupled via the thiol group of Cys. Cys-HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR, and also functions as a cytotoxic agent, cellular uptake inhibitor, and tumor growth inhibitor. Cys-HW12 is applicable to pancreatic cancer-related research .
POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer .
Dicatenarin is a caspase‑3 activator with growth‑inhibitory activity against human cancer cells. Dicatenarin increases caspase‑3 activity, induces intracellular ROS generation, and activates the mitochondrial‑mediated apoptotic pathway. Dicatenarin exerts growth‑inhibitory effects against a panel of human cancer cell lines. Dicatenarin can be used in research on pancreatic cancer, lung cancer, colon cancer, breast cancer, prostate cancer, and ovarian cancer .
HW12 is a random peptide containing an N-terminal cysteine and is not an EGFR ligand. HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR. HW12 is applicable to pancreatic cancer-related research .
Anticancer agent 327, a fluorescent Andrographolide (HY-N0191) derivative, is an NF-κB p50 inhibitor. Anticancer agent 327 covalently binds to the p50 subunit of NF-κB. Anticancer agent 327 reduces levels of multiple oncogenic p53 proteins via the autophagy/lysosome pathway. Anticancer agent 327 can be used for the research of pancreatic ductal adenocarcinoma (Ex/Em = 488/515 nm)[1].
KRAS G12C-IN-76 (Compound 39) is an orally active KRAS G12C inhibitor. KRAS G12C-IN-76 inhibits the phosphorylation of ERK. KRAS G12C-IN-76 exhibits anticancer activity against pancreatic cancer .
Chlorin e6 is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer .
Chlorin e6 (solution) (Ce6 (solution)) is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer . Solvent and concentration: DMSO: 10 mM The 1 mL volume is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research .
ADT-1004 is an orally active prodrug of ADT-007 (HY-157887). ADT-007 is a reversible, highly potent and selective pan-RAS inhibitor that binds to the nucleotide-free conformation of RAS proteins and blocks their GTP activation, thereby inhibiting the downstream MAPK and AKT signaling pathways. ADT-1004 can be used for the research of pancreatic ductal adenocarcinoma .
N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide (Compound L3) is a thiourea ligand and monodentate ligand. The IC50 of N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide in tested cell lines is > 100 μM. N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide shows no activity against colorectal cancer cells and pancreatic cancer cells .
Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
Copper (II) pyrithione is a New Delhi metallo-β-lactamase 1 inhibitor. Copper (II) pyrithione inhibits New Delhi metallo-β-lactamase 1 via transmetallation of its zinc (II) cofactor with copper (II). Copper (II) pyrithione exerts cytotoxic effects on pancreatic cancer cells and osteosarcoma cells. Copper (II) pyrithione exhibits antibacterial activity against Gram-positive bacteria and some Gram-negative bacteria. Copper (II) pyrithione can synergistically enhance the activity of β-lactam antibiotics against β-lactam-resistant bacteria. Copper (II) pyrithione can be used in studies related to pancreatic cancer, osteosarcoma and bacterial infections .
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
Mecbotamab vedotin (BA3011) is a pH dependent antibody drug conjugate (ADC) targeting AXL. Mecbotamab vedotin can significantly inhibit AXL in DU145 cells and LCLC-103H cells and kills cells. Mecbotamab vedotin can be used for research on cancer such as lung cancer, pancreatic cancer and prostate cancer. The antibody component is Mecbotamab (HY-P9988), and the ADC toxin molecule is Monomethyl auristatin E (MMAE) (HY-15162) .
H2S probe 1 (compound 1NND) is a derivative of nitrobenzoxadiazole (NBD) with antitumor activity. H2S probe 1 is cytotoxic to human pancreatic cancer cell MIA PaCa-2 (IC50=77.9 nM) and has a high affinity for human telomeric G-quadruplex (G4) (Kd=1.72 μM). H2S probe 1 can be used in cancer research .
Chlorin e6 (solution) (Ce6 (solution)) is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer . Solvent and concentration: DMSO: 10 mM The 1 mL volume is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors .
Dodecapeptide AR71 is an inhibitor of melanoma inhibitory activity (MIA). Dodecapeptide AR71 can reduce cell migration, reduce metastasis formation, and increase immune response. Dodecapeptide AR71 can be used in research on the treatment of malignant melanoma .
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells .
Cys-HW12 is a random peptide containing an N-terminal cysteine. Cys-HW12 can be coupled via the thiol group of Cys. Cys-HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR, and also functions as a cytotoxic agent, cellular uptake inhibitor, and tumor growth inhibitor. Cys-HW12 is applicable to pancreatic cancer-related research .
HW12 is a random peptide containing an N-terminal cysteine and is not an EGFR ligand. HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR. HW12 is applicable to pancreatic cancer-related research .
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
Tomentosin is an orally active natural sesquiterpenoid lactone. Tomentosin exhibits multiple activities such as anti-tumor, anti-fungal, anti-inflammatory, anti-oxidant and neuroprotective effects. Tomentosin can inhibit tumor cell proliferation, migration and invasion, and induce apoptosis. Tomentosin can be used in the research of tumors, inflammation and nervous system diseases .
Geranic acid (Geranate) acts as a tyrosinase inhibitor and antifungal agent, with an IC50 value of 0.14-2.3 mM against mushroom tyrosinase. Geranic acid reduces the viability of human pancreatic cancer cells and B-lymphoma cells. Geranic acid inhibits mycelial growth of the maize pathogens Colletotrichum graminicola and Fusarium graminearum. Geranic acid is applicable to research related to fungal infections, pancreatic cancer and B-lymphoma .
Foryshiyanine A is a triterpenoid alkaloid. Foryshiyanine A possesses anti-inflammatory activity, inhibiting the release of β-glucuronidase from rat polymorphonuclear leukocytes. Foryshiyanine A exhibits antiviral activity, with an EC50 of 4.5 μM against respiratory syncytial virus (RSV) and an IC50 of 7.3 μM against influenza A virus (H1N1). Foryshiyanine A reduces viral load by disrupting viral replication and entry. Foryshiyanine A may be used for the researches of inflammation and infection .
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells .
Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2 .
Dicatenarin is a caspase‑3 activator with growth‑inhibitory activity against human cancer cells. Dicatenarin increases caspase‑3 activity, induces intracellular ROS generation, and activates the mitochondrial‑mediated apoptotic pathway. Dicatenarin exerts growth‑inhibitory effects against a panel of human cancer cell lines. Dicatenarin can be used in research on pancreatic cancer, lung cancer, colon cancer, breast cancer, prostate cancer, and ovarian cancer .
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (His) is the recombinant human-derived MIA protein, expressed by E. coli , with C-6*His labeled tag.
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (N-His) is the recombinant human-derived MIA protein, expressed by E. coli , with N-6*His labeled tag.
CKMT1A is a creatine kinase isoenzyme that plays a key role in the reversible transfer of phosphate between ATP and creatine phosphate. The function of this enzyme is critical for tissues with dynamic energy needs, such as skeletal muscle, heart, brain, and sperm. CKMT1A Protein, Human (sf9, His) is the recombinant human-derived CKMT1A protein, expressed by Sf9 insect cells , with N-His labeled tag.
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
MIA Human Pre-designed siRNA Set A contains three designed siRNAs for MIA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mia gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
MIA2 Human Pre-designed siRNA Set A contains three designed siRNAs for MIA2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
MIA3 Human Pre-designed siRNA Set A contains three designed siRNAs for MIA3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mia2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia Rat Pre-designed siRNA Set A contains three designed siRNAs for Mia gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mia2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Mia2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Otor Mouse Pre-designed siRNA Set A contains three designed siRNAs for Otor gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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