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MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .
DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
N,N-Dimethyl-idarubicin-trisaccharide (compound 26) is an efficient intercalating agent. N,N-Dimethyl-idarubicin-trisaccharide shows excellent cytotoxicity against ABCG2-overexpressing and ABCB1-overexpressing cells with IC50s of 19 and 32 nM, respectively .
PNMT-IN-1 (inhibtor 4) is a specific inhibitor of phenylethanolamine N-methyltransferas (PNMT) with a Ki value of 1.2 nM and a IC50 value of 81 nM.
PNMT-IN-1 also inhibits the vitality of DNMT1 and DNMT3b, with the IC50 value of 61 μM and 17 μM, respectively, and has an antagonistic effect on epinephrine.PNMT-IN-1 (inhibtor 4 ) is a second generation inhibitor .
Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
Gancotamab (MM-302) is a HER2-targeted antibody-liposomal Doxorubicin conjugate with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells .
PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models .
N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells .
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
KY386 is a potent, selective inhibitor of DHX33 helicase, with the IC50 of 19 nM. KY386 inhibits U251-MG cells (DHX33-overexpressing cancer cell strain) with IC50 of 20 nM.and shows potent anti-cancer activity and moderate metabolic stability .
GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models .
CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells .
MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .
SSO111 sodium, a 20mer fully modified antisense oligonucleotide, targets the oncogene?HER2. SSO111 sodium induces exon 15 skipping during splicing, leading to the generation of a novel mRNA transcript that excludes exon 15. SSO111 sodium downregulated HER2 mRNA, which resulted in the inhibition of proliferation and induction of apoptosis in HER2-overexpressing tumor cells.
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .
Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells .
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
BTA-EG4 is a catalase-amyloid interaction inhibitor, which can significantly enhance the neurotoxicity of amyloid peptides in catalase-overexpressing neuronal cells, and can be used in the study of neurodegenerative diseases .
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
TTX-P is a fluorescent probe. TTX-P responds in situ to the overexpressed alkaline phosphatase (ALP) in liver, imaging of diabetic liver injury in the near-infrared second-window (NIR-II) region .
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
Anticancer agent 198 (compound 18b) is a potent anticancer agent and potential WRN protein inhibitor. Anticancer agent 198 was significantly toxic to K562 cells and WRN-overexpressing PC3 cells .
Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells .
2-Deoxy-L-ribose is a stereoisomer of 2-Deoxy-d-ribose that inhibits 2-Deoxy-d-ribose anti-apoptotic effects. 2-Deoxy-L-ribose suppresses metastasis of tumor cells overexpressing thymidine phosphorylase .
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
CG-707 inhibits phosphatase of regenerating liver-3 (PRL-3) enzymatic activity with an IC50 value of 0.8 μM. CG-707 inhibits the migration and invasion of PRL-3overexpressing colon cancer cells .
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
NOTA-FAPI-52 is a tracer with potent tumor uptake. NOTA-FAPI-52 can be radiolabeled to enable PET imaging or other bioimaging techniques. NOTA-FAPI-52 can be used to study diseases in which fibroblast activation protein (FAP) is overexpressed .
Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .
DSPE-PEG5000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
SIC5-6 is a potent Separase inhibitor. Separase, a large cysteine protease, involves in chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, spindle stabilization and elongation. Separase is highly overexpressed in many solid cancers, serves as an attractive chemotherapeutic target .
Tenatumomab (ST2146) is a murine monoclonal antibody against tenascin-C. And tenascin-C, the large extracellular glycoprotein, is overexpressed in cancer. Tenatumomab has been used for Pretargeted Antibody Guided Radioimmunoresearch (PAGRIT), and delivering radionuclides to tumors via PAGRIT and direct 131Iodine labeling approach .
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYCoverexpressing cancer cells to CDK4/6 inhibitors .
DSPE-PEG2000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG2000-pPB can be used for drug delivery .
DSPE-PEG2000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG2000-GE11 can be used for drug delivery .
CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6 .
DSPE-PEG1000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG1000-pPB can be used for drug delivery .
DSPE-PEG1000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG1000-GE11 can be used for drug delivery .
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM .
DSPE-PEG5000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG5000-pPB can be used for drug delivery .
BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) inducer and antiviral agent. BEPP hydrochloride effectively inhibits the growth of human lung cancer cell lines overexpressingPKR and induces apoptosis and activates caspase-3 in sensitive cells. In addition, BEPP hydrochloride can also significantly inhibit vaccinia virus replication .
Bodilisant is a fluorescent histamine H3 receptor ligand. Bodilisant can be used at low concentrations (1-10 nM) to detect the performance of hH3R in cells overexpressing hH3R, and at about 1 μM concentration for tissues rich in hH3R. Bodilisant is a useful pharmacological tool for receptor imaging .
P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYCoverexpressing cancer cells to CDK4/6 inhibitors .
Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A. Aurora A has been implicated in cancers of diverse histological origin and may possess oncogenic properties when overexpressed. Aurora A inhibitor 1 has the potential for the research of cancer diseases mediated by aurora a (extracted from patent WO2021147974A1, compound 49) .
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases .
Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases .
H2-005 is a compound that selectively inhibits diacylglycerol acyltransferase 2 (DGAT2) and has the activity to inhibit triacylglycerol synthesis in hepatocytes and preadipocytes. H2-005 significantly reduces triacylglycerol biosynthesis in HepG2 hepatocytes and 3T3-L1 preadipocytes. H2-005 exhibits specific inhibitory activity in DGAT2-overexpressing HEK293 cells. H2-005 almost completely inhibits lipid droplet formation in 3T3-L1 cells when co-treated with a DGAT1 inhibitor. H2-005 will contribute to DGAT2-related lipid metabolism research and the development of drugs to inhibit metabolic diseases .
9,10-trans-Dehydroepothilone D shows an antiproliferative activity against a paclitaxel-resistant cell lines overexpressingP-glycoprotein. 9,10-trans-Dehydroepothilone D also shows tubulin polymerization activity. 9,10-trans-Dehydroepothilone D is given by lactonization of Seco acid, which is promising for research of cancers .
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK .
RUSKI-201 dihydrochloride is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 0.20 μM. RUSKI-201 dihydrochloride is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 dihydrochloride is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function .
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD + required for rapid proliferation. MS7, as a NAMPT target protein ligand, can be used to synthesize PROTAC A7, which is an effective NAMPT degrader. MS7 can be used in cancer research .
PHGDH-IN-5 (Compound B12) is a covalen inhibitor of PHGDH with an IC50 value of 0.29 μM. PHGDH-IN-5 can inhibit cell proliferation in cancer cell lines overexpressingPHGDH. PHGDH-IN-5 can reduce the production of serine derived from glucose in MDA-MB-468 cells .
RUSKI-201 is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor, with an IC50 of 0.20 μM. RUSKI-201 is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function .
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXLoverexpressing renal cell carcinomas .
TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .
Acid Ceramidase-IN-2 (compound 1) is an acid ceramidase inhibitor with potentially antiproliferative and cytostatic activities. Moreover, human acid ceramidase is overexpressed in prostate cancer cells, indicating potential anti-tumor effect of Acid Ceramidase-IN-2. And Acid Ceramidase-IN-2 hydrolysis can be inhibited by 3 a-ketoamides GT85, GT98 and GT99 inhibits in vitro .
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
CaMdr1p-IN-1 (Compound A) is an inhibitor for the major facilitator superfamily transporter CaMdr1p. CaMdr1p-IN-1 exhibits chemosensitizing efficacy. CaMdr1p-IN-1 synergizes with Fluconazole (HY-B0101), that inhibits CaMdr1p overexpressingCandida albicans with MIC of 10 μM .
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .
SPI-001 is a PPM1D-specific inhibitor (IC50=0.48 μM) with anticancer activity. SPI-001 inhibits PPM1D phosphatase activity and increases p53 phosphorylation in PPM1D-overexpressing human breast cancer cells. In addition, SPI-001 inhibits cell proliferation by inducing apoptosis .
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
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 .
4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease .
Bcl-2-IN-22 (compound 1) is a gold(I) NHC complex with anticancer activity. Bcl-2-IN-22 induces apoptosis via the mitochondrial pathway with an IC50 value of 0.014 μM. In addition, Bcl-2-IN-22 targets BCL-2 family members and exhibits pro-apoptosis and resensitization properties in multidrug-resistant leukemia cells that overexpressBCL?2 .
AP-4-139B is a heat shock protein 70 inhibitor (IC50=180 nM). HSP70 is a protein that is overexpressed in many types of cancer and is closely related to the survival and proliferation of tumor cells. AP-4-139B exhibits significant cytotoxicity to tumor cells, particularly in colorectal cancer cells. AP-4-139B can be used for cancer research .
Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
Tamrintamab (SC-003 mAb, SC-Mab003, SC34.28ss1) is an ADC Antibody targeting to dipeptidase 3 (DPEP3 or MBD3). DPEP3 is a glycosyl phosphatidylinositol anchored metallopeptidase that is overexpressed in ovarian tumors. Tamrintamab can specifically bind DPEP3-expressing cells to produce cytotoxicity. Tamrintamab can be used in ovarian cancer research .
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A) .
[Leu15]-Gastrin I (human) is a Leu15-labeled Gastrin I (human) peptide hormone, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
APHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition .
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
NDM-1 inhibitor-2 is an inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) and has the ability to inhibit NDM-1 activity. NDM-1 inhibitor-2 exhibits a good inhibitory effect on drug-resistant bacterial strains that overexpress NDM-1. When NDM-1 inhibitor-2 is used in combination with the carbapenem antibiotic meropenem, a favorable synergistic effect can be produced .
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells .
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2overexpressed tumor models .
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
TTX-P is a fluorescent probe. TTX-P responds in situ to the overexpressed alkaline phosphatase (ALP) in liver, imaging of diabetic liver injury in the near-infrared second-window (NIR-II) region .
2-Deoxy-L-ribose is a stereoisomer of 2-Deoxy-d-ribose that inhibits 2-Deoxy-d-ribose anti-apoptotic effects. 2-Deoxy-L-ribose suppresses metastasis of tumor cells overexpressing thymidine phosphorylase .
DSPE-PEG5000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
DSPE-PEG2000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG2000-pPB can be used for drug delivery .
DSPE-PEG2000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG2000-GE11 can be used for drug delivery .
DSPE-PEG1000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG1000-pPB can be used for drug delivery .
DSPE-PEG1000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG1000-GE11 can be used for drug delivery .
DSPE-PEG5000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG5000-pPB can be used for drug delivery .
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .
[Leu15]-Gastrin I (human) is a Leu15-labeled Gastrin I (human) peptide hormone, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
CPK peptide is a tumor-localizing peptide. CPK peptide specifically binds to the monocarboxylate transporter 1 (MCT1) receptor, which is overexpressed in many human colon cancer cell lines but not in normal cells. CPK peptide can be used in tumor diagnosis research .
MAGE-3 (271-279) is a 271-279 residue peptide derived from melanoma antigens encoded by MAGE-3. MAGE-3 is a cytolytic T lymphocyte (CTL)-defined MAGE-3 protein associated with the human leukocyte antigen (HLA)-A2 molecule. MAGE-3 is overexpressed in different human tumor types, including malignant melanoma, but not by normal tissues except for testis and placenta .
Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
Letaplimab (IBI-188) is a human IgG4 anti-CD47 monoclonal antibody. CD47 is overexpressed on cancer cells, it is a ligand for SIRPα. Letaplimab enhances tumor cell phagocytosis .
Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
Tenatumomab (ST2146) is a murine monoclonal antibody against tenascin-C. And tenascin-C, the large extracellular glycoprotein, is overexpressed in cancer. Tenatumomab has been used for Pretargeted Antibody Guided Radioimmunoresearch (PAGRIT), and delivering radionuclides to tumors via PAGRIT and direct 131Iodine labeling approach .
Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXLoverexpressing renal cell carcinomas .
Tamrintamab (SC-003 mAb, SC-Mab003, SC34.28ss1) is an ADC Antibody targeting to dipeptidase 3 (DPEP3 or MBD3). DPEP3 is a glycosyl phosphatidylinositol anchored metallopeptidase that is overexpressed in ovarian tumors. Tamrintamab can specifically bind DPEP3-expressing cells to produce cytotoxicity. Tamrintamab can be used in ovarian cancer research .
Gancotamab (MM-302) is a HER2-targeted antibody-liposomal Doxorubicin conjugate with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells .
Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells .
Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells .
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM .
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 .
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
ANO1/Anoctamin-1 protein, a calcium-activated chloride channel (CaCC), is involved in ion transport, smooth muscle contraction, and mucus secretion. ANO1/Anoctamin-1 Protein, Human (N-His, C-Myc) is the recombinant human-derived ANO1/Anoctamin-1 protein, expressed by E. coli , with C-Myc, N-10*His labeled tag.
NOV/CCN3 Protein belongs to an emerging family of growth regulators referred under the CCN acronym. NOV/CCN3 Protein enables heparin and binding. NOV/CCN3 Protein is involved in cell adhesion and signal transduction. NOV/CCN3 Protein, Canine (HEK293, His) is the recombinant canine-derived NOV/CCN3 protein, expressed by HEK293 , with C-His labeled tag. The total length of NOV/CCN3 Protein, Canine (HEK293, His) is 325 a.a., with molecular weight of 42-50 KDa.
NOV/CCN3 proteins perform a wide range of functions, including proliferation, adhesion, migration, differentiation, and survival. It interacts with various proteins, such as integrins and membrane receptors, affecting different cellular responses. NOV/CCN3 Protein, Human (sf9, His) is the recombinant human-derived NOV/CCN3 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of NOV/CCN3 Protein, Human (sf9, His) is 326 a.a., with molecular weight of approximately 47 kDa.
The NOV/CCN3 protein is an early player that coordinates diverse cellular processes such as proliferation, adhesion, migration, differentiation, and survival.By interacting with membrane receptors such as integrins or NOTCH1, it regulates hematopoietic stem cells and inhibits myogenic differentiation while affecting the expression of cell cycle regulators.NOV/CCN3 Protein, Mouse (HEK293, His) is the recombinant mouse-derived NOV/CCN3 protein, expressed by HEK293 , with C-6*His labeled tag.
Insulin-like growth factor 2 mRNA-binding protein 3; IGF2 mRNA-binding protein 3; IMP-3; IGF-II mRNA-binding protein 3; KH domain-containing protein Overexpressed in cancer (hKOC); VICKZ family member 3; IGF2BP3; IMP3; KOC1; VICKZ3
NOV/CCN3 proteins are involved in a variety of biological processes, including migration, differentiation, survival, and inflammation. It acts by binding to integrins or membrane receptors such as NOTCH1. NOV/CCN3 Protein, Rhesus Macaque (sf9, His) is the recombinant Rhesus Macaque-derived NOV/CCN3 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of NOV/CCN3 Protein, Rhesus Macaque (sf9, His) is 326 a.a., with molecular weight of ~37.2 KDa.
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
SSO111 sodium, a 20mer fully modified antisense oligonucleotide, targets the oncogene?HER2. SSO111 sodium induces exon 15 skipping during splicing, leading to the generation of a novel mRNA transcript that excludes exon 15. SSO111 sodium downregulated HER2 mRNA, which resulted in the inhibition of proliferation and induction of apoptosis in HER2-overexpressing tumor cells.
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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