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SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive ligand of SETdomain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD .
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SETdomain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SETdomain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest .
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SETdomain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SETdomain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .
BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SETdomain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
BI-9321 is a potent, selective and cellular active nuclear receptor-binding SETdomain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SETdomain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .
AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 µM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SETdomain, with the Kd value of 0.78 µM .
MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease .
MMSET-IN-1 is a multiple myeloma SETdomain(MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET .
NSD-IN-3 (compound 3) is a potent nuclear receptor binding SETdomain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
Ryuvidine is a potent inhibitor of SETdomain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro . Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells .
UNC8153 TFA is a potent and selective nuclear receptor-binding SETdomain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SETdomain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SETdomain (Kd of 370 nM) .
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SETdomain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SETdomain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .
T-cell immunoreceptor with Ig and ITIM domains; VSIG9; VSTM3; TIGIT; V-SET and transmembrane domain-containing protein 3; V-SET and immunoglobulin domain-containing protein 9
Ig-like domain-containing protein is a class of proteins that may be involved in protein–protein and protein–ligand interactions, therefore being involved in biological processes such as down-regulation of T cell activation or cardiac and neuronal development. TIGIT Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived TIGIT protein, expressed by HEK293 , with C-6*His labeled tag. The total length of TIGIT Protein, Cynomolgus (HEK293, His) is 121 a.a., with molecular weight of 16-30 kDa.
T-cell immunoreceptor with Ig and ITIM domains; ; VSIG9; VSTM3; TIGIT; V-SET and transmembrane domain-containing protein 3; V-SET and immunoglobulin domain-containing protein 9
The TIGIT protein plays a key role in immune regulation and binds with high affinity to the poliovirus receptor (PVR). This interaction induces an immunosuppressive environment by increasing IL10 secretion and decreasing IL12B secretion. TIGIT Protein, Human (HEK293, mFc) is the recombinant human-derived TIGIT protein, expressed by HEK293 , with C-mFc labeled tag. The total length of TIGIT Protein, Human (HEK293, mFc) is 120 a.a., with molecular weight of 40-50 kDa.
T-cell immunoreceptor with Ig and ITIM domains; ; VSIG9; VSTM3; TIGIT; V-SET and transmembrane domain-containing protein 3; V-SET and immunoglobulin domain-containing protein 9
The TIGIT protein plays a key role in immune regulation and binds with high affinity to the poliovirus receptor (PVR). This interaction induces an immunosuppressive environment by increasing IL10 secretion and decreasing IL12B secretion. TIGIT Protein, Human (120a.a, HEK293, His) is the recombinant human-derived TIGIT protein, expressed by HEK293 , with C-6*His labeled tag. The total length of TIGIT Protein, Human (120a.a, HEK293, His) is 120 a.a., with molecular weight of 16-18 kDa.
T-cell immunoreceptor with Ig and ITIM domains; VSIG9; VSTM3; TIGIT; V-SET and transmembrane domain-containing protein 3; V-SET and immunoglobulin domain-containing protein 9
Ig-like domain-containing protein is a class of proteins that may be involved in protein–protein and protein–ligand interactions, therefore being involved in biological processes such as down-regulation of T cell activation or cardiac and neuronal development. TIGIT Protein, Cynomolgus (HEK293, C-hFc) is the recombinant cynomolgus-derived TIGIT protein, expressed by HEK293 , with C-hFc labeled tag. The total length of TIGIT Protein, Cynomolgus (HEK293, C-hFc) is 121 a.a., with molecular weight of 45-55 kDa.
Chromosome 11 open reading frame 90; CK090 HUMAN; Uncharacterized protein C11orf90; V SET and transmembrane domain containing 5; V-SET and transmembrane domain-containing protein 5
The VSTM5 protein acts as a cell adhesion-like membrane protein in the central nervous system (CNS) and exerts a critical influence on the positioning and complexity of central neurons by regulating their membrane morphology and dynamics. It is actively involved in the formation of neuronal dendrites and protrusions, including dendritic filopodia, contributing to the complex structure of neural networks. VSTM5 Protein, Human (His) is the recombinant human-derived VSTM5 protein, expressed by E. coli , with N-His labeled tag. The total length of VSTM5 Protein, Human (His) is 119 a.a., with molecular weight of ~19.3 kDa.
V-set and immunoglobulin domain containing 4 (Vsig4) is a membrane protein belonging to complement receptor of the immunoglobulin superfamily. Vsig4 may be a negative regulator of T-cell responses and interleukin-2 production, Vsig4 also mediates clearance of C3b opsonized pathogens by binding C3b. The expression of VSIG4 is restricted to tissue macrophages where Vsig4 inhibits proinflammatory macrophage activation by reprogramming mitochondrial pyruvate metabolism. VSIG4 Protein, Mouse (168a.a, HEK293, His) is the recombinant mouse-derived VSIG4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of VSIG4 Protein, Mouse (168a.a, HEK293, His) is 168 a.a., with molecular weight of 28-35 kDa.
V-set and immunoglobulin domain-containing protein 8 (VSIG8) is a membrane protein belonging to complement receptor of the immunoglobulin superfamily. VSIG8 has RNA binding activity and is a human T-cell co-inhibitory ligand. VSIG-8 inhibits the production of cytokines, chemokines and other proteins on T cells, and also suppresses T cell proliferation and differentiation of na茂ve T cells. VSIG8 Protein, Human (HEK293, Fc) is the recombinant human-derived VSIG8 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of VSIG8 Protein, Human (HEK293, Fc) is 242 a.a., with molecular weight of ~57.0 kDa.
V-set and immunoglobulin domain-containing protein 8 (VSIG8) is a membrane protein belonging to complement receptor of the immunoglobulin superfamily. VSIG8 has RNA binding activity and is a human T-cell co-inhibitory ligand. VSIG-8 inhibits the production of cytokines, chemokines and other proteins on T cells, and also suppresses T cell proliferation and differentiation of na茂ve T cells. VSIG8 Protein, Human (HEK293, His) is the recombinant human-derived VSIG8 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of VSIG8 Protein, Human (HEK293, His) is 242 a.a., with molecular weight of 28-35 kDa.
VSTM2A Protein, a key player in early white and brown preadipocyte differentiation, actively promotes adipogenic commitment by upregulating the transcription factor PPARG. This regulatory role operates within a BMP4-dependent signaling pathway, highlighting intricate molecular mechanisms in differentiation. Additionally, VSTM2A functions as a homodimer, suggesting involvement in complex protein-protein interactions critical for its regulatory activities. VSTM2A Protein, Human ( E84K, HEK293, His) is the recombinant human-derived VSTM2A protein, expressed by HEK293 , with C-6*His labeled tag and E84K mutation. The total length of VSTM2A Protein, Human ( E84K, HEK293, His) is 220 a.a., with molecular weight of 38-40 kDa.
VSIG2 is also known as CTXL (cortical thymocyte like-protein). VSIG2 promotes malignant progression of pancreatic ductal adenocarcinoma through LAMtor2-mediated mTOR activation. VSIG2 can be used as a potential biomarker or therapeutic target for tumors. VSIG2 Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived VSIG2 protein, expressed by HEK293, with C-His labeled tag. The total length of VSIG2 Protein, Human (Biotinylated, HEK293, His) is 220 a.a., with molecular weight of ~24.6 kDa.
V-set and immunoglobulin domain containing 4 (Vsig4) is a membrane protein belonging to complement receptor of the immunoglobulin superfamily. Vsig4 may be a negative regulator of T-cell responses and interleukin-2 production, Vsig4 also mediates clearance of C3b opsonized pathogens by binding C3b. The expression of VSIG4 is restricted to tissue macrophages where Vsig4 inhibits proinflammatory macrophage activation by reprogramming mitochondrial pyruvate metabolism. VSIG4 Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived VSIG4 protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of VSIG4 Protein, Mouse (HEK293, His-Fc) is 187 a.a., with molecular weight of ~60 kDa.
VSIG4 Protein, a phagocytic receptor, robustly inhibits T-cell proliferation and IL2 production, serving as a potent alternative complement pathway convertase inhibitor. VSIG4 Protein, Human (HEK293, Fc) is the recombinant human-derived VSIG4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of VSIG4 Protein, Human (HEK293, Fc) is 265 a.a., with molecular weight of ~75.0 kDa.
VSTM1 interacts with S100A10 protein, inducing the dimerization of ANXA2/p36. This suggests a regulatory role in protein phosphorylation, with ANXA2 monomer being the preferred target for tyrosine-specific kinase in vitro. The resulting heterotetramer comprises two light chains of S100A10/p11 and two heavy chains of ANXA2/p36. Furthermore, VSTM1 engages with SCN10A and TASOR, indicating its participation in diverse molecular interactions. VSTM1 Protein, Human (HEK293, Fc) is the recombinant human-derived VSTM1 protein, expressed by HEK293, with C-hFc labeled tag. The total length of VSTM1 Protein, Human (HEK293, Fc) is 135 a.a., with molecular weight of 50-60 kDa.
VSIG2 is also known as CTXL (cortical thymocyte like-protein). VSIG2 promotes malignant progression of pancreatic ductal adenocarcinoma through LAMtor2-mediated mTOR activation. VSIG2 can be used as a potential biomarker or therapeutic target for tumors. VSIG2 Protein, Human (HEK293, His) is the recombinant human-derived VSIG2 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of VSIG2 Protein, Human (HEK293, His) is 220 a.a., with molecular weight of 29-35 kDa.
VSIG4 Protein, a phagocytic receptor, robustly inhibits T-cell proliferation and IL2 production, serving as a potent alternative complement pathway convertase inhibitor. VSIG4 Protein, Human (264a.a, HEK293, His) is the recombinant human-derived VSIG4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of VSIG4 Protein, Human (264a.a, HEK293, His) is 264 a.a., with molecular weight of ~50.0 kDa.
VSTM1 interacts with S100A10 protein, inducing the dimerization of ANXA2/p36. This suggests a regulatory role in protein phosphorylation, with ANXA2 monomer being the preferred target for tyrosine-specific kinase in vitro. The resulting heterotetramer comprises two light chains of S100A10/p11 and two heavy chains of ANXA2/p36. Furthermore, VSTM1 engages with SCN10A and TASOR, indicating its participation in diverse molecular interactions. VSTM1 Protein, Human (119a.a, HEK293, His) is the recombinant human-derived VSTM1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of VSTM1 Protein, Human (119a.a, HEK293, His) is 119 a.a., with molecular weight of 25-35 kDa.
TIGIT protein, with signaling receptor binding activity, functions upstream of T cell activation suppression. Active on the cell surface, it shares orthology with human TIGIT. Associated with modulating T cell responses, TIGIT exhibits biased expression, notably in the large intestine, small intestine, and other tissues. This highlights its potential in immune regulation within these contexts. TIGIT Protein, Mouse (110a.a, HEK293, His) is the recombinant mouse-derived TIGIT protein, expressed by HEK293 , with C-6*His labeled tag. The total length of TIGIT Protein, Mouse (110a.a, HEK293, His) is 110 a.a., with molecular weight of 15-22 kDa.
The B7-H4 protein acts as a negative regulator and inhibits T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. Significant significance can be observed when expressed on tumor macrophages, cooperating with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Mouse (sf9, His) is the recombinant mouse-derived B7-H4 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of B7-H4 Protein, Mouse (sf9, His) is 228 a.a., with molecular weight of ~26.6 kDa.
The B7-H4 protein acts as a negative regulator and inhibits T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. Significant significance can be observed when expressed on tumor macrophages, cooperating with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Mouse (HEK293, His) is 228 a.a., with molecular weight of ~26.6 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (HEK293, His) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Human (HEK293, His) is 230 a.a., with molecular weight of 43-48 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity and create an immunosuppressive microenvironment. B7-H4 Protein, Rat (HEK293, His) is the recombinant rat-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Rat (HEK293, His) is 228 a.a., with molecular weight of 42-65 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Human (Biotinylated, HEK293, His) is 230 a.a., with molecular weight of ~26.8 KDa.
B7-H4 Protein, Mouse (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
B7-H4 Protein, Human (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
B7-H4 Protein, Rhesus macaque (HEK293, His) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
B7-H4 Protein, Rhesus macaque (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (Biotinylated, HEK293, Fc-Avi) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-Avi, C-hFc labeled tag. The total length of B7-H4 Protein, Human (Biotinylated, HEK293, Fc-Avi) is 230 a.a., with molecular weight of 70-95 kDa.
