PRMT

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S7748	EPZ015666 (GSK3235025)	<1 mg/mL	60 mg/mL	'48 mg/mL
S8147	MS049	56 mg/mL	56 mg/mL	50 mg/mL
S8340	SGC2085	<1 mg/mL	62 mg/mL	62 mg/mL
S7820	EPZ020411 2HCl	81 mg/mL	100 mg/mL	''100 mg/mL
S7832	SGC707	<1 mg/mL	59 mg/mL	59 mg/mL
S8112	MS023	<1 mg/mL	57 mg/mL	57 mg/mL
S8883	LLY-283	5 mg/mL	68 mg/mL	3 mg/mL
S5445	AMI-1 (free acid)	-1 mg/mL	20 mg/mL	'-1 mg/mL
S8664	Pemrametostat (GSK3326595)	<1 mg/mL	90 mg/mL	'90 mg/mL
S8111	GSK591	<1 mg/mL	76 mg/mL	76 mg/mL
S8209	HLCL-61 HCL	<1 mg/mL	76 mg/mL	76 mg/mL
S8624	Onametostat (JNJ-64619178)	-1 mg/mL	100 mg/mL	'-1 mg/mL
S8858	GSK3368715 (EPZ019997) 3HCl	81 mg/mL	81 mg/mL	'81 mg/mL
S0855	TC-E 5003	<1 mg/mL	80 mg/mL	'<1 mg/mL
S7884	AMI-1	10 mg/mL	100 mg/mL	<1 mg/mL
S6737	C7280948	<1 mg/mL	55 mg/mL	5 mg/mL
S0184	XY1	˂1 mg/mL	59 mg/mL	1 mg/mL

亜型選択性的な製品

PRMT製品

All (17) PRMT阻害剤(16)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S7748	EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i of 5 nM, >20,000-fold selectivity over other PMTs.	Sci Adv, 2021, 7(13)eabc1834 Front Immunol, 2021, 12:695947 Ann Transl Med, 2021, 9(9):755	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.	Research Square, 2021, 10.21203/rs.3.rs-620216/v1 EMBO Rep, 2020, 21(2):e48597
S8340	SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
S7820^新	EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.	Theranostics, 2020, 10(1):133-150
S7832	SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and K_d of 31 nM and 53 nM, respectively.	J Med Chem, 2020, 31 Transpl Int, 2020, 33(2):229-243 J Immunother Cancer, 2019, 7(1):277
S8112	MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Proteome Sci, 2020, 19;18:6
S8883	LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
S5445	AMI-1 (free acid) AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S8664	Pemrametostat (GSK3326595) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.	Sci Adv, 2021, 7(13)eabc1834 Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118 Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8111	GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.	Hepatology, 2021, 10.1002/hep.32245 Cancer Sci, 2021, 10.1111/cas.14988 Elife, 2020, 9e57617	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
S8209	HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.	Nat Commun, 2018, 9(1):1572 Cancer Res, 2018, 78(20):5731-5740
S8624	Onametostat (JNJ-64619178) Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.	Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8858	GSK3368715 (EPZ019997) 3HCl GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Ki^app vaules ranging from 1.5 to 81 nM.
S0855	TC-E 5003 TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
S7884	AMI-1 AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Research Square, 2021, 10.21203/rs.3.rs-620216/v1	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
S6737	C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389
S0184	XY1 XY1 is an inactive, close analog of SGC707 that can be used as the negative control for SGC707. SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S7748	EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i of 5 nM, >20,000-fold selectivity over other PMTs.	Sci Adv, 2021, 7(13)eabc1834 Front Immunol, 2021, 12:695947 Ann Transl Med, 2021, 9(9):755	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.	Research Square, 2021, 10.21203/rs.3.rs-620216/v1 EMBO Rep, 2020, 21(2):e48597
S8340	SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
S7820^新	EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.	Theranostics, 2020, 10(1):133-150
S7832	SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and K_d of 31 nM and 53 nM, respectively.	J Med Chem, 2020, 31 Transpl Int, 2020, 33(2):229-243 J Immunother Cancer, 2019, 7(1):277
S8112	MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Proteome Sci, 2020, 19;18:6
S8883	LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
S5445	AMI-1 (free acid) AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S8664	Pemrametostat (GSK3326595) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.	Sci Adv, 2021, 7(13)eabc1834 Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118 Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8111	GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.	Hepatology, 2021, 10.1002/hep.32245 Cancer Sci, 2021, 10.1111/cas.14988 Elife, 2020, 9e57617	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
S8209	HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.	Nat Commun, 2018, 9(1):1572 Cancer Res, 2018, 78(20):5731-5740
S8624	Onametostat (JNJ-64619178) Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.	Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8858	GSK3368715 (EPZ019997) 3HCl GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Ki^app vaules ranging from 1.5 to 81 nM.
S0855	TC-E 5003 TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
S7884	AMI-1 AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Research Square, 2021, 10.21203/rs.3.rs-620216/v1	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
S6737	C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S0184	XY1 XY1 is an inactive, close analog of SGC707 that can be used as the negative control for SGC707. SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S0184

XY1

XY1 is an inactive, close analog of SGC707 that can be used as the negative control for SGC707. SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

研究分野別

製品類型

PRMT

阻害剤の選択性比較

亜型選択性的な製品

PRMT製品

EPZ015666 (GSK3235025)

MS049

SGC2085

EPZ020411 2HCl

SGC707

MS023

LLY-283

AMI-1 (free acid)

Pemrametostat (GSK3326595)

GSK591

HLCL-61 HCL

Onametostat (JNJ-64619178)

GSK3368715 (EPZ019997) 3HCl

TC-E 5003

AMI-1

C7280948

XY1