目录号 | 产品详情 | 靶点 | |
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T12266 | Tyrosine Kinases JAK | ||
Ilginatinib (NS-018) 是一种可口服的JAK2强效抑制剂,IC50值为 0.72 nM,对其选择性是对 JAK1、JAK3和 Tyk2 的 46、54 和 22 倍,IC50分别为 33、39 和 22 nM。 | |||
T22416 | Tyrosine Kinases JAK | ||
RO495 (CS-2667) 是一种有效的非受体酪氨酸蛋白激酶2抑制剂。 | |||
T3072 | Apoptosis FLT JAK PDGFR | ||
XL019 是一种具有口服活性的选择性JAK2抑制剂。它对JAK2的选择性是 100 多种丝氨酸/苏氨酸和酪氨酸激酶的 50 倍以上。它对 JAK2 V617F 和野生型 JAK2 细胞中 STAT3 和 STAT5 磷酸化有抑制作用。 | |||
T15096 | Tyrosine Kinases JAK | ||
Delgocitinib(JTE-052)是一种特异性的JAK(Janus激酶)抑制剂,其对JAK1、JAK2、JAK3 和 Tyk2 的 IC50 值分别为 2.8、2.6、13 和 58 nM。Delgocitinib 通过JAK-依赖性细胞因子参与多种炎症和自身免疫性疾病,能有效地遏制多种细胞因子信号传递,同时抑制了因细胞因子而引发的瘙痒。它可广泛用于治疗各种炎症性疾病,包括自身免疫性疾病和超敏反应。 | |||
T6S1966 | Antioxidant NF-κB JAK STAT | ||
Curculigoside (Curculigoside A) 是仙茅中的主要皂苷,具有显著的抗氧化、抗骨质疏松、抗抑郁和神经保护作用。它通过调节JAK/STAT/NF-κB 信号传导途径,具有抗关节炎作用。 | |||
T79110 | JAK | ||
JAK-IN-27(化合物1)是JAK家族激酶的口服有效抑制剂,对TYK2、JAK1和JAK3的IC50分别为3.0 nM、7.7 nM和629.6 nM。此外,JAK-IN-27能够抑制Jurkat细胞内由IFN-α2B诱导的STAT3磷酸化,其IC50为23.7 nM。 | |||
T7503 | JAK | ||
Upadacitinib (ABT-494) 是高效选择性的,具有口服活性的 JAK1抑制剂,IC50为43 nM,可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。 | |||
T3998 | JAK | ||
Itacitinib (INCB039110) 是一种选择性 JAK1抑制剂,对 人JAK1的IC50值为 2 nM。它对JAK1选择性是 JAK2 的 20 倍多,是 JAK3 和 TYK2 的 100 倍多。 | |||
T3076 | Tyrosine Kinases JAK | ||
GLPG0634 analog (GLPG0634 analogue) 是一种 JAK 广谱性抑制剂,对 JAK1/JAK2/JAK3 的 IC50值为 50 到 200 nM 之间。 | |||
T6321 | ROCK Apoptosis JAK Src | ||
Tofacitinib (Tasocitinib) 是口服小分子 Janus 激酶抑制剂,用于治疗中度至重度类风湿性关节炎。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-02273 | JAK1 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors.
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TMPH-02274 | JAK2 Protein, Human, Recombinant (His) | Human | E. coli | ||
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin.
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TMPH-02961 | JAK1 Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors. JAK1 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 39.1 kDa and the accession number is P52332.
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TMPH-02272 | JAK1 Protein, Human, Recombinant (E. coli, His) | Human | E. coli | ||
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors.
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TMPK-00474 | IL-22RA1 Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
IL-22 receptor, also known as IL-22 R alpha 1 and CRF2-9, is an approximately 65 kDa transmembrane glycoprotein in the type II cytokine receptor family (CRF).Component of the receptor for IL20, IL22 and IL24. Component of IL22 receptor formed by IL22RA1 and IL10RB enabling IL22 signaling via JAK/STAT pathways. IL22 also induces activation of MAPK1/MAPK3 and Akt kinases pathways. Component of one of the receptor for IL20 and IL24 formed by IL22RA1 and IL20RB also signaling through STATs activation. Mediates IL24 antiangiogenic activity as well as IL24 inhibitory effect on endothelial cell tube formation and differentiation.
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TMPJ-00059 | IL-7 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Human Interleukin 7 (IL-7) is a potent lymphoid cell growth factor stimulating the proliferation of lymphoid progenitors. IL7 can associate with the hepatocyte growth factor (HGF) to form a hybrid cytokine that functions as a pre-pro-B cell growth-stimulating factor. Human IL7 cDNA encodes a 177 amino acid precursor protein containing a 25 amino acid signal peptide and a 152 amino acid mature protein. Human and mouse IL7 share 65% sequence identity in the mature region and both exhibit cross-species activity. IL-7 signals via IL-7 receptor (IL7R) activating multiple pathways including JaK/STAT and PI3K/AKT, which regulate lymphocyte survival, glucose uptake, proliferation, and differentiation. IL-7 is also associated with cytoplasmic IL2-R gamma for signal transduction.
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TMPH-00779 | IL-23 P19/IL23A Protein, Guinea Pig, Recombinant (His & Myc) | Guinea pig | E. coli | ||
Associates with IL12B to form the IL-23 interleukin, a heterodimeric cytokine which functions in innate and adaptive immunity. IL-23 may constitute with IL-17 an acute response to infection in peripheral tissues. IL-23 binds to a heterodimeric receptor complex composed of IL12RB1 and IL23R, activates the Jak-Stat signaling cascade, stimulates memory rather than naive T-cells and promotes production of proinflammatory cytokines. IL-23 induces autoimmune inflammation and thus may be responsible for autoimmune inflammatory diseases and may be important for tumorigenesis.
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TMPJ-00076 | IL-28B Protein, Human, Recombinant | Human | HEK293 Cells | ||
Interleukin-28B, also known as Cytokine Zcyto22, Interferon lambda-3, Interferon lambda-4, IFNL3, IFNL4, ZCYTO22 and IL28B, is a secreted cytokine which belongs to the IL-28/IL-29 family. IL-28 has also been shown to play a role in the adaptive immune response. IL28B has immunomodulatory activity and up-regulates MHC class I antigen expression. IL28B displays potent antiviral activity and antitumor activity. In addition, IL28B is a ligand for the heterodimeric class II cytokine receptor composed of IL10RB and IL28RA. The ligand/receptor complex seems to signal through the Jak-STAT pathway.
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TMPK-01071 | IL-22RA1 Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Interleukin (IL)-22 is a member of the IL-10 family of cytokines and represents an important effector molecule of activated Th22, Th1, and Th17 cells, as well as Tc-cell subsets, gammadelta T cells, natural killer (NK), and NKT cells. IL-22 mediates its effects via a heterodimeric transmembrane receptor complex consisting of IL-22R1 and IL-10R2 and subsequent Janus kinase-signal transducers and activators of transcription (JAK-STAT) signaling pathways including Jak1, Tyk2, and STAT3. IL-22RA1 Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 51.1 kDa and the accession number is Q80XZ4.
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TMPU-00003 | STAT2 Protein, Human, Recombinant (His) | Human | E. coli | ||
Signal transducer and activator of transcription that mediates signaling by type I IFNs (IFN-alpha and IFN-beta). Following type I IFN binding to cell surface receptors, Jak kinases (TYK2 and JAK1) are activated, leading to tyrosine phosphorylation of STAT1 and STAT2. The phosphorylated STATs dimerize, associate with ISGF3G/IRF-9 to form a complex termed ISGF3 transcription factor, that enters the nucleus. ISGF3 binds to the IFN stimulated response element (ISRE) to activate the transcription of interferon stimulated genes, which drive the cell in an antiviral state.
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TMPK-01105 | IL-22RA1 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Interleukin (IL)-22 is a member of the IL-10 family of cytokines and represents an important effector molecule of activated Th22, Th1, and Th17 cells, as well as Tc-cell subsets, gammadelta T cells, natural killer (NK), and NKT cells. IL-22 mediates its effects via a heterodimeric transmembrane receptor complex consisting of IL-22R1 and IL-10R2 and subsequent Janus kinase-signal transducers and activators of transcription (JAK-STAT) signaling pathways including Jak1, Tyk2, and STAT3. IL-22RA1 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 51 kDa and the accession number is Q8N6P7.
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TMPH-01551 | IFNLR1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
The IFNLR1/IL10RB dimer is a receptor for the cytokine ligands IFNL2 and IFNL3 and mediates their antiviral activity. The ligand/receptor complex stimulate the activation of the JAK/STAT signaling pathway leading to the expression of IFN-stimulated genes (ISG), which contribute to the antiviral state. Determines the cell type specificity of the lambda interferon action. Shows a more restricted pattern of expression in the epithelial tissues thereby limiting responses to lambda interferons primarily to epithelial cells of the respiratory, gastrointestinal, and reproductive tracts. Seems not to be essential for early virus-activated host defense in vaginal infection, but plays an important role in Toll-like receptor (TLR)-induced antiviral defense. Plays a significant role in the antiviral immune defense in the intestinal epithelium.
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TMPJ-00326 | CD122/IL2RB Protein, Human, Recombinant (aa 27-239, His & Avi), Biotinylated | Human | HEK293 Cells | ||
Human IL-2RB, also known asinterleukin-2 receptor subunit beta,is the receptor for interleukin-2. IL2 receptor complex is involved in receptor mediated endocytosis and transduces the mitogenic signals of IL2. IL2 receptor complex has three forms with respect to ability to bind IL2. IL-2RB is belonged to a type I membrane protein,and has a 26 residue signal peptide, a 214 residue extracellular region, a 25 residue transmembrane region and a 286 residue cytoplasmic domain. IL-2RB is the subunit critical for receptor-mediated signaling via physically or functionally coupling to other signaling molecules, such as the Jak-STAT and Src-family protein tyrosine kinase although it lacks apparent catalytic motifs.
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TMPH-02156 | SOCS1 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
SOCS family proteins form part of a classical negative feedback system that regulates cytokine signal transduction. SOCS1 is involved in negative regulation of cytokines that signal through the JAK/STAT pathway. Through binding to JAKs and IFNGR1, inhibits their kinase activity. In vitro, also suppresses Tec protein-tyrosine activity. Appears to be a major regulator of signaling by interleukin 6 (IL6) and leukemia inhibitory factor (LIF). Regulates interferon-gamma mediated sensory neuron survival. Probable substrate recognition component of an ECS (Elongin BC-CUL2/5-SOCS-box protein) E3 ubiquitin ligase complex which mediates the ubiquitination and subsequent proteasomal degradation of target proteins. Seems to recognize JAK2. SOCS1 appears to be a negative regulator in IGF1R signaling pathway.
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TMPY-02624 | IL-9R Protein, Rat, Recombinant (His) | Rat | HEK293 Cells | ||
IL9R (Interleukin 9 Receptor) is a Protein Coding gene. The protein encoded by this gene is a cytokine receptor that specifically mediates the biological effects of interleukin 9 (IL9). IL9 is involved in mast cell maturation and the enhancement of IgE production by B cells. Furthermore, linkage data in the human and mice have suggested that IL9 may contribute to asthma. The ligand binding of this receptor leads to the activation of various JAK kinases and STAT proteins, which connect to different biologic responses. IL9R is known to be autosomal in mice and is X-linked only in primates. The more recent X linkage and more telomeric position of the IL9R gene may explain its autosomal, 'un-inactivated' transcriptional status.
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TMPJ-00194 | IL-20RB Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Interleukin-20 receptor subunit beta(IL20RB) is a single-pass type I membrane protein and belongs to the type II cytokine receptor family. It contains 2 fibronectin type-III domains. There are two kinds of type II cytokine receptors : cytokine receptors that bind type I and type II interferons; cytokine receptors that bind members of the interleukin-10 family (interleukin-10, interleukin-20 and interleukin-22). Type II cytokine receptors are similar to type I cytokine receptors except they do not possess the signature sequence WSXWS that is characteristic of type I receptors. They are expressed on the surface of certain cells, which bind and respond to a select group of cytokines. These receptors are related predominantly by sequence similarities in their extracellular portions that are composed of tandem Ig-like domains. The intracellular domain of type II cytokine receptors is typically associated with a tyrosine kinase belonging to the Janus kinase (JAK) family.
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TMPY-02194 | SOCS3 Protein, Human, Recombinant (His & Trx) | Human | E. coli | ||
Suppressor of cytokine signaling 3, also known as SOCS-3, Cytokine-inducible SH2 protein 3, CIS-3, STAT-induced STAT inhibitor 3, SOCS3 and CIS3, is a protein which is widely expressed with high expression in heart, placenta, skeletal muscle, peripheral blood leukocytes, fetal and adult lung, and fetal liver and kidney. SOCS3 / CIS3 contains one SH2 domain and one SOCS box domain. SOCS family proteins form part of a classical negative feedback system that regulates cytokine signal transduction. SOCS3 / CIS3 is involved in negative regulation of cytokines that signal through the JAK / STAT pathway. SOCS3 / CIS3 inhibits cytokine signal transduction by binding to tyrosine kinase receptors including gp13, LIF, erythropoietin, insulin, IL12, GCSF and leptin receptors. Binding to JAK2 inhibits its kinase activity. SOCS3 / CIS3 suppresses fetal liver erythropoiesis. It regulates onset and maintenance of allergic responses mediated by T-helper type 2 cells. SOCS3 / CIS3 regulates IL-6 signaling. SOCS3 / CIS3 interacts with multiple activated proteins of the tyrosine kinase signaling pathway including IGF1 receptor, insulin receptor and JAK2. SOCS3 / CIS3 could be used as a possible therapeutic agent for treating rheumatoid arthritis.
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TMPJ-01003 | STAT5B Protein, Human, Recombinant (His) | Human | E. coli | ||
Signal Transducer and Activator of Transcription 5b (STAT5B) is a member of the STAT family of transcription factors. They are responsible for an array of cellular activities including regulating growth, survival, differentiation, motility, and the immune response. STAT5B mediates the signal transduction triggered by various cell ligands, such as IL2, IL4, CSF1, and different growth hormones. It has been shown to be involved in diverse biological processes, such as TCR signaling, apoptosis, adult mammary gland development, and sexual dimorphism of liver gene expression. Signal transduction and activator of transcription 5 (STAT5) is a member of the Jak/STAT signal transduction pathway and is activated by a variety of cytokines (IL22, IL6). STAT5 has two isoforms (A and B) that share 93% amino acid identity and bind the DNA consensus site TTCN3GAA. STAT5 mediates cytokine signaling by acting as a signal transducer in the cytoplasm and, upon phosphorylation, translocates to the nucleus and activates transcription of specific genes. STAT5 is involved in a wide array of biological processes ranging from regulating apoptosis to adult mammary gland proliferation, differentiation and survival.
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TMPJ-00495 | ISG15 Protein, Human, Recombinant (His) | Human | E. coli | ||
Ubiquitin-Like Protein ISG15 (ISG15) is a ubiquitin-like protein that becomes conjugated to many cellular proteins upon activation by interferon-alpha and -beta. Several functions have been ascribed to the encoded protein, including chemotactic activity towards neutrophils, direction of ligated target proteins to intermediate filaments, cell-to-cell signaling, and antiviral activity during viral infections. While conjugates of this protein have been found to be noncovalently attached to intermediate filaments, this protein is sometimes secreted. ISG15 becomes conjugated to a diverse set of proteins after IFN-alpha/beta stimulation or microbial challenge. The functions or biochemical consequences ISG15 conjugation to proteins are not yet known, but it appears that this modification does not target proteins for proteasomal degradation. ISG15 shows specific chemotactic activity towards neutrophils and activates them to induce release of eosinophil chemotactic factors. Upon interferon treatment, ISG15 can be detected in both free and conjugated forms, and is secreted from monocytes and lymphocytes where it can function as a cytokine. In the cell, ISG15 co-localizes with intermediate filaments and ISGylation may modulate the JAK-STAT pathway or certain aspects of neurological disease.
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TMPY-04084 | ANGPTL1 Protein, Canine, Recombinant (hFc) | Canine | HEK293 Cells | ||
Angiopoietin-like protein 1 (ANGPTL1) has been reported to suppress migration and invasion in lung and breast cancer, acting as a novel tumor suppressor candidate. Downregulation of tumor suppressor signaling plays an important role in the pathogenesis of hepatocellular carcinoma (HCC).The downregulation of the angiopoietin-like protein ANGPTL1 is associated with vascular invasion, tumor thrombus, metastasis, and poor prognosis in HCC. Ectopic expression of ANGPTL1 in HCC cells effectively decreased their in vitro and in vivotumorigenicity, cell motility, and angiogenesis. shRNA-mediated depletion of ANGPTL1 exerted opposing effects. ANGPTL1 promoted apoptosis via inhibition of the STAT3/Bcl-2-mediated antiapoptotic pathway and decreased cell migration and invasion via downregulation of transcription factors SNAIL and SLUG. Furthermore, ANGPTL1 inhibited angiogenesis by attenuating ERK and AKT signaling and interacted with integrin α1β1 receptor to suppress the downstream FAK/Src-JAK-STAT3 signaling pathway. Taken together, these results suggest ANGPTL1 as a prognostic biomarker and novel therapeutic agent in HCC. ANGPTL1 expression was down-regulated in CRC tissues and inversely correlated with poor survival. ANGPTL1 repressed migration and invasion of CRC cells, and microRNA-138 was involved in this process. Angiopoietin-like protein 1 (ANGPTL1) has been shown to act as a tumor suppressor by inhibiting angiogenesis, cancer invasion, and metastasis.
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TMPH-00775 | IFN gamma Protein, Goat, Recombinant (His & Myc) | Goat | E. coli | ||
Type II interferon produced by immune cells such as T-cells and NK cells that plays crucial roles in antimicrobial, antiviral, and antitumor responses by activating effector immune cells and enhancing antigen presentation. Primarily signals through the JAK-STAT pathway after interaction with its receptor IFNGR1 to affect gene regulation. Upon IFNG binding, IFNGR1 intracellular domain opens out to allow association of downstream signaling components JAK2, JAK1 and STAT1, leading to STAT1 activation, nuclear translocation and transcription of IFNG-regulated genes. Many of the induced genes are transcription factors such as IRF1 that are able to further drive regulation of a next wave of transcription. Plays a role in class I antigen presentation pathway by inducing a replacement of catalytic proteasome subunits with immunoproteasome subunits. In turn, increases the quantity, quality, and repertoire of peptides for class I MHC loading. Increases the efficiency of peptide generation also by inducing the expression of activator PA28 that associates with the proteasome and alters its proteolytic cleavage preference. Up-regulates as well MHC II complexes on the cell surface by promoting expression of several key molecules such as cathepsins B/CTSB, H/CTSH, and L/CTSL. Participates in the regulation of hematopoietic stem cells during development and under homeostatic conditions by affecting their development, quiescence, and differentiation.
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