目录号 | 产品详情 | 靶点 | |
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T9969 | Histone Methyltransferase | ||
EZM0414 是一种有效、选择性、口服生物利用度高的SETD2抑制剂,在 SETD2 生化分析中,IC50值为18 nM;在细胞分析中,IC50值为34 nM。EZM0414可用于复发或难治性多发性骨髓瘤和弥漫性大 B 细胞淋巴瘤的研究。 | |||
T3398 | Apoptosis JAK STAT Autophagy | ||
Icaritin (Anhydroicaritin) 是Epimedium Genusis 的异戊二烯类黄酮衍生物,有效抑制 K562 细胞和原代 CML 细胞的增殖。它可以调节MAPK/ERK/JNK 和JAK2/STAT3/AKT 信号传导,并具有增强成骨的作用。 | |||
T72979 | Histone Methyltransferase | ||
LEM-14-1189 是一种 LEM-14 衍生物,是一种有效的核受体结合SET结构域 NSD 抑制剂,对 NSD1、NSD2、NSD3 具有抑制作用,IC50 分别为 418 μM 、111 μM 和 60 μM 。LEM-14-1189 具有潜在的抗癌活性,可用于研究多发性骨髓瘤 (MM)和血液系统疾病。 | |||
T76794 | Apoptosis CXCR | ||
Ulocuplumab (BMS-936564) 是一种完全人 抗 CXCR4 的 IgG4 抗体。Ulocplumab 在急性髓系白血病 (AML),非霍奇金淋巴瘤 (NHL) 和多发性骨髓瘤移植模型中展现出抗肿瘤活性。Ulocplumab 对 CXCL12 介导的慢性淋巴细胞白血病 (CLL) 细胞在 CXCR4 激活下的迁移有抑制作用,诱导癌细胞凋亡 (apoptosis),。 | |||
T6739 | Apoptosis Rho Autophagy | ||
Zoledronic Acid (ZOL 446) 是一种含氮二磷酸盐,能抑制破骨细胞的分化和凋亡,具有高效的抗骨质再吸收活性,也有抗癌作用。 | |||
T38951 | Apoptosis CD38 | ||
Isatuximab 是一种在血液系统恶性细胞中靶向跨膜受体和胞外酶 CD38 的单克隆抗体,是在多发性骨髓瘤中高度表达的蛋白。Isatuximab 具有抗肿瘤活性、抗体依赖性细胞介导的细胞毒性、补体依赖性细胞毒性、抗体依赖性细胞吞噬作用,可在无交联情况下直接诱导细胞凋亡 (apoptosis)。Isatuximab 对 CD38 胞外酶活性有抑制作用,这与许多细胞功能有关。 | |||
T35610 | Apoptosis Wnt/beta-catenin Prostaglandin Receptor | ||
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T28498L | Apoptosis | ||
rac-CCT-250863 HCl 是一种具有选择性和可逆性的 NEK 2 抑制剂。rac-CCT-250863 HCl 能诱导细胞周期停滞,对癌细胞有较好的抗增殖活性,与 Pomalidomide 联用能诱导细胞凋亡,可用于联合抗癌的研究。 | |||
T12083 | Others | ||
MMSET-IN-1 is an inhibitor of multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) . | |||
T10518 | Others | ||
BET-BAY 002 is an effective BET inhibitor and exhibits efficacy in a multiple myeloma model. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00331 | IFNAR1 Protein, Rhesus macaque, Recombinant (His) | Rhesus | HEK293 Cells | ||
Interferon‑alpha/beta receptor 1 (IFN‑ alpha / beta R1), also known as IFNAR1, are present in all tissues and even on the surface of most IFN-resistant cells. Isoform 1, isoform 2 and isoform 3 are expressed in the IFN-alpha sensitive myeloma cell line U266B1. Isoform 2 and isoform 3 are expressed in the IFN-alpha resistant myeloma cell line U266R. Isoform 1 is not expressed in IFN-alpha resistant myeloma cell line U266R. It interacts with STAT1 and STAT2, the interaction requires its phosphorylation at Tyr-466. It also interacts with FBXW11, the substrate recognition component of a SCF (SKP1-CUL1-F-box protein) E3 ubiquitin-protein ligase complex.
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TMPK-01035 | SP17 Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Sperm protein 17 (Sp17) is a highly conserved mammalian protein characterized in rabbit, mouse, monkey, baboon, macaque, human testis and spermatozoa. mRNA encoding Sp17 has been detected in a range of murine and human somatic tissues. It was also recognized in two myeloma cell lines and in neoplastic cells from patients with multiple myeloma and ovarian carcinoma. SP17 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-His tag. The predicted molecular weight is 18.39 kDa and the accession number is Q62252.
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TMPK-00974 | SP17 Protein, Human, Recombinant (His) | Human | E. coli | ||
Sperm protein 17 (Sp17) is a highly conserved mammalian protein characterized in rabbit, mouse, monkey, baboon, macaque, human testis and spermatozoa. mRNA encoding Sp17 has been detected in a range of murine and human somatic tissues. It was also recognized in two myeloma cell lines and in neoplastic cells from patients with multiple myeloma and ovarian carcinoma. SP17 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-His tag. The predicted molecular weight is 18.50 kDa and the accession number is Q15506.
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TMPK-00358 | CD229 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 Cells | ||
CD229 was strongly and homogeneously overexpressed on the PC of patients with monoclonal gammopathy of undetermined significance (MGUS), smoldering myeloma, MM, and PC leukemia. CD229 was particularly overexpressed on those PC showing an abnormal phenotype such as expression of CD56. Most importantly, CD229 was also highly expressed on those cells in the patients' BM displaying the phenotype of chemotherapy-resistant and myeloma-propagating cells. CD229 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 47.7 kDa and the accession number is Q9HBG7-1.
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TMPK-00357 | CD229 Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
CD229 was strongly and homogeneously overexpressed on the PC of patients with monoclonal gammopathy of undetermined significance (MGUS), smoldering myeloma, MM, and PC leukemia. CD229 was particularly overexpressed on those PC showing an abnormal phenotype such as expression of CD56. Most importantly, CD229 was also highly expressed on those cells in the patients' BM displaying the phenotype of chemotherapy-resistant and myeloma-propagating cells. CD229 Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 47.7 kDa and the accession number is Q9HBG7-1.
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TMPY-04409 | GRK6 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
G protein-coupled receptor kinase 6, also known as G protein-coupled receptor kinase GRK6, GRK6, and GPRK6, is a lipid-anchor protein that belongs to the protein kinase superfamily, AGC Ser/Thr protein kinase family, and GPRK subfamily. GRK6 / GPRK6 contains one AGC-kinase C-terminal domain, one protein kinase domain, and one RGS domain. This protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. Several transcript variants encoding different isoforms have been described. GRK6 / GPRK6 is widely expressed. GRK6 / GPRK6 silencing causes suppression of signal transducer and activator of transcription 3 (STAT3) phosphorylation associated with a reduction in MCL1 levels and phosphorylation, illustrating a potent mechanism for the cytotoxicity of GRK6 inhibition in multiple myeloma (MM) tumor cells. GRK6 also appears to be involved in responses to morphine. Inhibition of GRK6 represents a uniquely targeted novel therapeutic strategy in human multiple myeloma.
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TMPK-01193 | GPRC5D Protein-VLP, Mouse, Recombinant | Mouse | HEK293 Cells | ||
Chimeric antigen receptor (CAR) T cells, a type of cell-based immunotherapy, have shown some promising results in multiple myeloma, a bone marrow cancer.The orphan G protein–coupled receptor, class C group 5 member D (GPRC5D), normally expressed only in the hair follicle, Using quantitative immunofluorescence, we determined that GPRC5D protein is expressed on CD138 MM cells from primary marrow samples with a distribution that was similar to, but independent of, BCMA. GPRC5D Protein-VLP, Mouse, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 39.90 kDa and the accession number is Q9JIL6-1.
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TMPK-00528 | GPRC5D Protein-VLP, Cynomolgus, Recombinant | Cynomolgus | HEK293 Cells | ||
Chimeric antigen receptor (CAR) T cells, a type of cell-based immunotherapy, have shown some promising results in multiple myeloma, a bone marrow cancer.The orphan G protein–coupled receptor, class C group 5 member D (GPRC5D), normally expressed only in the hair follicle, Using quantitative immunofluorescence, we determined that GPRC5D protein is expressed on CD138 MM cells from primary marrow samples with a distribution that was similar to, but independent of, BCMA. GPRC5D Protein-VLP, Cynomolgus, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 35.10 kDa and the accession number is A0A2K5W6I7.
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TMPY-02924 | RGS1 Protein, Human, Recombinant (His) | Human | E. coli | ||
RGS1 (regulator of G-protein signaling 1) has been associated with multiple autoimmune disorders including type I diabetes. RGS1 desensitizes the chemokine receptors CCR7 and CXCR4 that are critical to the localization of T and B cells in lymphoid organs. RGS1 expression may be a prognostic marker for risk stratification and a promising target for the development of a new Multiple myeloma (MM) therapy. The markers in the RGS1 gene might be in linkage disequilibrium with a protective allele that reduces the risk of anxiety and depressive disorders.
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TMPJ-00291 | IL-6R alpha/CD126 Protein, Human, Recombinant (Avi & His), Biotinylated | Human | HEK293 Cells | ||
Interleukin 6 is a potent pleiotropic cytokine that regulates cell growth and differentiation and plays an important role in the immune response. IL6Ra is a part of the receptor for interleukin 6 cytokine. IL6Ra binds to IL6 with low affinity, but does not transduce a signal. Signal activation necessitates an association with IL6ST. Activation may lead to the regulation of the immune response, acute-phase reactions and hematopoiesis. Low concentration of a soluble form of IL6 receptor acts as an agonist of IL6 activity. Dysregulated production of IL6 and this receptor are implicated in the pathogenesis of many diseases, such as multiple myeloma, autoimmune diseases and prostate cancer.
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TMPJ-00130 | SLAMF2 Protein, Human, Recombinant (hFc & His) | Human | HEK293 Cells | ||
CD48 antigen, also known as B-lymphocyte activation marker BLAST-1, BCM1 surface antigen, Leukocyte antigen MEM-102, TCT.1, CD48, BCM1,and BLAST1, CD48 contains one Ig-like C2-type domain and one Ig-like V-type domain, but does not have a transmembrane domain, however, but is held at the cell surface by a GPI anchor via a C-terminal domain which maybe cleaved to yield a soluble form of the receptor. CD48 may facilitate interaction between activated lymphocytes and be involved in regulating T-cell activation. CD48 plays a vital role as an environmental sensor for regulating progenitor cell numbers and inhibiting tumor development. It is suggested that the anti-CD48 mAb has the potential to become an effective therapeutic mAb against multiple myeloma.
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TMPJ-00694 | BRD4 Protein, Human, Recombinant (His & Flag) | Human | E. coli | ||
Bromodomain-containing protein 4 (BRD4) is a member of the BET class chromatin reader proteins that bind acetylated histones and play a key role in transcriptional regulation and transmission of epigenetic memory. Remains associated with acetylated chromatin throughout the entire cell cycle and provides epigenetic memory for postmitotic G1 gene transcription by preserving acetylated chromatin status and maintaining high-order chromatin structure. BRD bromodomains serve as recognition motifs for acetylated lysine residues on histones, while the NET domain may function by promoting phosphorylation of the C-terminal domain (CTD) of RNA Polymerase II. Some specific inhibitors of BRD4 that prevent binding to acetylated histones by binding Asn-140 and Asn-433 are promising therapeutic molecules for the treatment of leukemias. BRD4 is a potential therapeutic target in many diseases including breast cancer, AML, multiple myeloma, colon cancer and others.
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TMPY-02843 | GPX7 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
GPX7 gene contains 3 distinct gt-ag introns. Transcription produces 4 different mRNAs, 3 alternatively spliced variants, and 1 unspliced form. There are 5 validated alternative polyadenylation sites. The mRNAs appear to differ by overlapping exons with different boundaries. GPX7 is an enzyme. It has molecular functions (glutathione peroxidase activity, oxidoreductase activity) and to localize in various compartments (extracellular space, extracellular region). GPX7 gene has been proposed to participate in pathways (Arachidonic acid metabolism, Glutathione metabolism), and processes (oxidation-reduction, response to oxidative stress). GPX7 modulates the bone turnover after ovariectomy in rats, it does not compensate for the action of estrogen after ovariectomy in rats. It has been shown that three mAbs (GPX7, GPX22, and GPZ35) inhibit IL-6-mediated biological responses such as Ig production in a human B cell line and proliferative responses of a human Lennert's lymphoma-derived T cell line, a human myeloma cell line, and a mouse pro-B cell line-derived transfectant expressing human gp130.
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TMPY-01710 | IkB alpha/NFKBIA Protein, Human, Recombinant (His) | Human | E. coli | ||
Nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (IkB alpha, NFKBIA, or IKBA), is a member of the NF-kappa-B inhibitor family that function to inhibit the NF-kB transcription factor. NFKBIA inhibits NF-kB by masking the nuclear localization signals (NLS) of NF-kB proteins and keeping them sequestered in an inactive state in the cytoplasm. Also, NFKBIA blocks the ability of NF-κB transcription factors to bind to DNA, which is required for NF-kB's proper functioning. Signal-induced degradation of I kappa B alpha exposes the nuclear localization signal of NF-kappa B, thus allowing it to translocate into the nucleus and activate transcription from responsive genes. An autoregulatory loop is established when NF-kappa B induces expression of the I kappa B alpha gene and newly synthesized I kappa B alpha accumulates in the nucleus where it negatively regulates NF-kappa B-dependent transcription. As part of this post-induction repression, the nuclear export signal on I kappa B alpha mediates the transport of NF-kappa B-I kappa B alpha complexes from the nucleus to the cytoplasm. Deletion of NFKBIA has an effect that is similar to the effect of EGFR amplification in the pathogenesis of glioblastoma and is associated with comparatively short survival. Polymorphisms in NFKBIA may be important in pre-disposition to and outcome after treatment, of multiple myeloma (MM). The NFKBIA gene product, IkappaBalpha, binds to NF-kappaB preventing its activation and is important in mediating resistance to apoptosis in B-cell lymphoproliferative diseases.
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