目录号 | 产品详情 | 靶点 | |
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T62907 | |||
TAS-117 hydrochloride 是一种选择性的、有效的、口服具有活力的别构 Akt 抑制剂,作用于 Akt1 (IC50: 4.8 nM) 、Akt2 (IC50: 1.6 nM) 和 Akt3 (IC50: 44 nM)。TAS-117 hydrochloride 能够激发抗骨髓瘤活性,增强蛋白酶体抑制诱导的致命内质网应激,可以诱导细胞凋亡和自噬。 | |||
T77084 | |||
Mezagitamab (TAK-079) 是一种 IgG1λ 类型的抗CD38单克隆抗体。其通过促进抗体和补体依赖性的细胞毒性,来耗尽表达CD38的肿瘤细胞,显示出在复发/难治性多发性骨髓瘤 (RRMM) 及原发性血小板减少性紫癜 (ITP) 等疾病中的治疗潜力。 | |||
T77127 | |||
Pacanalotamab (AMG 420;BI-836909) 是一种双特异性 T 细胞接合剂 (BiTE),靶向 BCMA 和 CD3ɛ。BCMA 是指 B 细胞成熟抗原,而 Pacanalotamab 会将 T 细胞重定向到细胞表面的 BCMA 表达细胞。Pacanalotamab 可对人多发性骨髓瘤 (MM) 细胞系进行 T 细胞重定向裂解。 | |||
T72989 | Apoptosis | ||
hGGPPS-IN-3(Compound 13h)是一种针对人类香叶基香叶基焦磷酸合成酶(hGGPPS)的有效抑制剂,属于C-2取代的噻吩并嘧啶基双膦酸盐(C2-ThP-BPs)衍生物。该化合物能够诱导多发性骨髓瘤(MM)细胞具有选择性地进入凋亡(apoptosis),并且在体内展现了对抗骨髓瘤的活性。 | |||
T63623 | |||
XPO1-IN-1 是口服具有活力的 XPO1 抑制剂,能够作用于 MM.1S 细胞 (IC50: 24 nM)。XPO1-IN-1 可以有效诱导细胞周期阻滞,并使细胞凋亡。XPO1-IN-1 表现出良好的代谢稳定性和药代动力学性质。XPO1-IN-1 能够用于研究多发性骨髓瘤。 | |||
T80762 | |||
XmAb 5592 是一款人源化Fc工程化的抗HM1.24抗体,通过增强与 FcγRIIIa 及 FcγRIIIb 受体的结合能力,增强了对HM1.24特异性多发性骨髓瘤(MM)细胞的抗体依赖性细胞毒性(ADCC)和抗体依赖性细胞吞噬(ADCP)作用,从而促进了体外裂解效果。 | |||
T11750 | Others | ||
KDOAM-25 citrate 是有效且具有高选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂,对 KDM5A,KDM5B,KDM5C,KDM5D 的IC50分别为 71 nM,19 nM,69 nM,69 nM。用KDOAM-25 citrate 处理的多发性骨髓瘤 MM1S 细胞显示转录起始位点的整体 H3K4 甲基化增加,增殖受损。 | |||
T62166 | |||
KDOAM-25 trihydrochloride 是一种有效的、高度选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂,能够作用于 KDM5A (IC50: 71 nM)、KDM5B (IC50: 19 nM)、KDM5C (IC50: 69 nM)、KDM5D (IC50: 69 nM)。KDOAM-25 trihydrochloride 能够提高转录起始位点的整体 H3K4 甲基化,可阻碍多发性骨髓瘤 MM1S 细胞的增殖。 | |||
T77033 | |||
Imvotamab (IGM-2323) 是一种具有双重作用机制的CD20xCD3双特异性IGM 抗体。Imvotamab 用于诱导生理性 T 细胞活化,以防止过度刺激和随后的免疫功能下调。Imvotamab 目前正被开发用于处理 B 细胞恶性肿瘤、多发性骨髓瘤 (MM) 和非霍奇金淋巴瘤 (NHL)。 | |||
T76995 | |||
Sotatercept (ACE-011) 是一种可溶性激活素受体 2A (ACVR2A) 型 IgGFc 融合蛋白。Sotatercept 结合了激活素和生长分化因子,试图恢复生长促进和生长抑制信号通路之间的平衡。Sotatercept 在肺动脉高压、贫血、骨质流失、红细胞生成、多发性骨髓瘤 (MM) 溶骨性病变中有潜在的应用。 |
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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