Chemicals
Showing 39151–39300 of 41137 results
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Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).
Brand:CaymanSKU:20700 -Available on backorder
Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).
Brand:CaymanSKU:20700 -Available on backorder
Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).
Brand:CaymanSKU:20700 -Available on backorder
Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}
Brand:CaymanSKU:-Available on backorder
Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}
Brand:CaymanSKU:-Available on backorder
Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}
Brand:CaymanSKU:-Available on backorder
Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}
Brand:CaymanSKU:-Out of stock
Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}
Brand:CaymanSKU:-Out of stock
Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}
Brand:CaymanSKU:-Out of stock
Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}
Brand:CaymanSKU:-Out of stock
Umirolimus is a semi-synthetic macrocyclic lactone and a derivative of rapamycin (Item No. 13346) that has immunosuppressive and anti-inflammatory effects.{36314} It halts the cell cycle at the G1 phase through an IL-2/mTOR-mediated pathway and inhibits proliferation of human smooth muscle cells. In a porcine overstretch model, coronary stents containing umirolimus for localized delivery to the vessel wall reduced stenosis by 50% and led to less thickening of the vessel wall than a bare metal stent. Rapamycin, and likely its derivatives, binds to the cytosolic FK-binding protein 12 (FKBP12) to inhibit the mammalian target of rapamycin (mTOR) pathway. Formulations containing umirolimus have been used in coronary stents for localized delivery to the vessel wall.
Brand:CaymanSKU:23585 - 1 mgAvailable on backorder
Umirolimus is a semi-synthetic macrocyclic lactone and a derivative of rapamycin (Item No. 13346) that has immunosuppressive and anti-inflammatory effects.{36314} It halts the cell cycle at the G1 phase through an IL-2/mTOR-mediated pathway and inhibits proliferation of human smooth muscle cells. In a porcine overstretch model, coronary stents containing umirolimus for localized delivery to the vessel wall reduced stenosis by 50% and led to less thickening of the vessel wall than a bare metal stent. Rapamycin, and likely its derivatives, binds to the cytosolic FK-binding protein 12 (FKBP12) to inhibit the mammalian target of rapamycin (mTOR) pathway. Formulations containing umirolimus have been used in coronary stents for localized delivery to the vessel wall.
Brand:CaymanSKU:23585 - 5 mgAvailable on backorder
UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}
Brand:CaymanSKU:-Available on backorder
UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}
Brand:CaymanSKU:-Available on backorder
UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}
Brand:CaymanSKU:-Available on backorder
UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}
Brand:CaymanSKU:-Available on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}
Brand:CaymanSKU:- The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}
Brand:CaymanSKU:- The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}
Brand:CaymanSKU:- The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}
Brand:CaymanSKU:-
SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}
Brand:CaymanSKU:-Out of stock
SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}
Brand:CaymanSKU:-Out of stock
SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}
Brand:CaymanSKU:-Out of stock
UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}
Brand:CaymanSKU:11084 - 1 mgAvailable on backorder
UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}
Brand:CaymanSKU:11084 - 10 mgAvailable on backorder
UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}
Brand:CaymanSKU:11084 - 25 mgAvailable on backorder
UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}
Brand:CaymanSKU:11084 - 5 mgAvailable on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:10734 - 1 mgAvailable on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:10734 - 10 mgAvailable on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:10734 - 5 mgAvailable on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:10734 - 50 mgAvailable on backorder
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-
G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}
Brand:CaymanSKU:11085 - 1 mgAvailable on backorder
G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}
Brand:CaymanSKU:11085 - 10 mgAvailable on backorder
G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}
Brand:CaymanSKU:11085 - 5 mgAvailable on backorder
G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}
Brand:CaymanSKU:11085 - 50 mgAvailable on backorder
UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20566 -Available on backorder
UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20566 -Available on backorder
UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20566 -Available on backorder
UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20566 -Available on backorder
Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}
Brand:CaymanSKU:-Out of stock
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}
Brand:CaymanSKU:-Out of stock
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}
Brand:CaymanSKU:-Out of stock
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}
Brand:CaymanSKU:-Out of stock
Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}
Brand:CaymanSKU:-Available on backorder
Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}
Brand:CaymanSKU:-Available on backorder
Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}
Brand:CaymanSKU:-Available on backorder
Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}
Brand:CaymanSKU:-Available on backorder
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 = 230 nM).{30116}
Brand:CaymanSKU:-Available on backorder
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 = 230 nM).{30116}
Brand:CaymanSKU:-Available on backorder
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 = 230 nM).{30116}
Brand:CaymanSKU:-Available on backorder
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 = 230 nM).{30116}
Brand:CaymanSKU:-Available on backorder
UNC2881 is an inhibitor of Mer (IC50 = 4.3 nM), a member of the TAM family of receptor tyrosine kinases.{45606} It is selective for Mer over the remaining TAM family members Axl and TYRO3 (IC50s = 360 and 250 nM, respectively). UNC2881 inhibits phosphorylation of Mer in 697 B-ALL acute lymphoblastic leukemia cells (IC50 = 21.9 nM). It inhibits platelet aggregation and ATP release induced by type I equine fibrillar collagen in isolated human platelet-rich plasma when used at a concentration of 3 μM.
Brand:CaymanSKU:29012 - 10 mgAvailable on backorder
UNC2881 is an inhibitor of Mer (IC50 = 4.3 nM), a member of the TAM family of receptor tyrosine kinases.{45606} It is selective for Mer over the remaining TAM family members Axl and TYRO3 (IC50s = 360 and 250 nM, respectively). UNC2881 inhibits phosphorylation of Mer in 697 B-ALL acute lymphoblastic leukemia cells (IC50 = 21.9 nM). It inhibits platelet aggregation and ATP release induced by type I equine fibrillar collagen in isolated human platelet-rich plasma when used at a concentration of 3 μM.
Brand:CaymanSKU:29012 - 25 mgAvailable on backorder
UNC2881 is an inhibitor of Mer (IC50 = 4.3 nM), a member of the TAM family of receptor tyrosine kinases.{45606} It is selective for Mer over the remaining TAM family members Axl and TYRO3 (IC50s = 360 and 250 nM, respectively). UNC2881 inhibits phosphorylation of Mer in 697 B-ALL acute lymphoblastic leukemia cells (IC50 = 21.9 nM). It inhibits platelet aggregation and ATP release induced by type I equine fibrillar collagen in isolated human platelet-rich plasma when used at a concentration of 3 μM.
Brand:CaymanSKU:29012 - 5 mgAvailable on backorder
UNC2881 is an inhibitor of Mer (IC50 = 4.3 nM), a member of the TAM family of receptor tyrosine kinases.{45606} It is selective for Mer over the remaining TAM family members Axl and TYRO3 (IC50s = 360 and 250 nM, respectively). UNC2881 inhibits phosphorylation of Mer in 697 B-ALL acute lymphoblastic leukemia cells (IC50 = 21.9 nM). It inhibits platelet aggregation and ATP release induced by type I equine fibrillar collagen in isolated human platelet-rich plasma when used at a concentration of 3 μM.
Brand:CaymanSKU:29012 - 50 mgAvailable on backorder
Phosphatidylinositol-4-phosphate 5-kinase type-1 γ (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG).{26548} Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2.{26548} UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM).{26548} It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases.{26548} At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw.{26548}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol-4-phosphate 5-kinase type-1 γ (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG).{26548} Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2.{26548} UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM).{26548} It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases.{26548} At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw.{26548}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol-4-phosphate 5-kinase type-1 γ (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG).{26548} Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2.{26548} UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM).{26548} It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases.{26548} At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw.{26548}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol-4-phosphate 5-kinase type-1 γ (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG).{26548} Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2.{26548} UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM).{26548} It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases.{26548} At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw.{26548}
Brand:CaymanSKU:-Out of stock
UNC3866 is an inhibitor of chromobox homolog 7 (CBX7; Kd = 97 nM).{30607} It also binds to CBX4 (Kd = 94 nM) but is greater than 6-fold selective over CBX2, 6, and 8 and the chromodomain Y family (CDY) chromodomains CDY1, L1b, and L2 (Kds = 0.61-6.3 μM). UNC3866 pretreatment (30 μM) of PC3 lysates completely inhibits chemiprecipitation of CBX7. It induces a senescent-like morphology and reduces growth of PC3 cells with an EC50 value of 7.6 μM.
Brand:CaymanSKU:-Available on backorder
UNC3866 is an inhibitor of chromobox homolog 7 (CBX7; Kd = 97 nM).{30607} It also binds to CBX4 (Kd = 94 nM) but is greater than 6-fold selective over CBX2, 6, and 8 and the chromodomain Y family (CDY) chromodomains CDY1, L1b, and L2 (Kds = 0.61-6.3 μM). UNC3866 pretreatment (30 μM) of PC3 lysates completely inhibits chemiprecipitation of CBX7. It induces a senescent-like morphology and reduces growth of PC3 cells with an EC50 value of 7.6 μM.
Brand:CaymanSKU:-Available on backorder
UNC3866 is an inhibitor of chromobox homolog 7 (CBX7; Kd = 97 nM).{30607} It also binds to CBX4 (Kd = 94 nM) but is greater than 6-fold selective over CBX2, 6, and 8 and the chromodomain Y family (CDY) chromodomains CDY1, L1b, and L2 (Kds = 0.61-6.3 μM). UNC3866 pretreatment (30 μM) of PC3 lysates completely inhibits chemiprecipitation of CBX7. It induces a senescent-like morphology and reduces growth of PC3 cells with an EC50 value of 7.6 μM.
Brand:CaymanSKU:-Available on backorder
UNC3866 is an inhibitor of chromobox homolog 7 (CBX7; Kd = 97 nM).{30607} It also binds to CBX4 (Kd = 94 nM) but is greater than 6-fold selective over CBX2, 6, and 8 and the chromodomain Y family (CDY) chromodomains CDY1, L1b, and L2 (Kds = 0.61-6.3 μM). UNC3866 pretreatment (30 μM) of PC3 lysates completely inhibits chemiprecipitation of CBX7. It induces a senescent-like morphology and reduces growth of PC3 cells with an EC50 value of 7.6 μM.
Brand:CaymanSKU:-Available on backorder
UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).{41372} It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Item No. 12092) and methotrexate (Item No. 13960). In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.{41373}
Brand:CaymanSKU:22966 - 1 mgAvailable on backorder
UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).{41372} It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Item No. 12092) and methotrexate (Item No. 13960). In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.{41373}
Brand:CaymanSKU:22966 - 10 mgAvailable on backorder
UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).{41372} It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Item No. 12092) and methotrexate (Item No. 13960). In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.{41373}
Brand:CaymanSKU:22966 - 25 mgAvailable on backorder
UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).{41372} It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Item No. 12092) and methotrexate (Item No. 13960). In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.{41373}
Brand:CaymanSKU:22966 - 5 mgAvailable on backorder
UNC669 is an inhibitor of the MBT domain of L3MBTL1 with an IC50 value of 6 µM.{19425} It is 5- and 10-fold selective for L3MBTL1 over the related proteins L3MBTL3 and L3MBTL4.
Brand:CaymanSKU:10875 - 10 mgAvailable on backorder
UNC669 is an inhibitor of the MBT domain of L3MBTL1 with an IC50 value of 6 µM.{19425} It is 5- and 10-fold selective for L3MBTL1 over the related proteins L3MBTL3 and L3MBTL4.
Brand:CaymanSKU:10875 - 25 mgAvailable on backorder
UNC669 is an inhibitor of the MBT domain of L3MBTL1 with an IC50 value of 6 µM.{19425} It is 5- and 10-fold selective for L3MBTL1 over the related proteins L3MBTL3 and L3MBTL4.
Brand:CaymanSKU:10875 - 5 mgAvailable on backorder