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CARM1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) HDAC (1) Histone Methyltransferase (20) Parasite (2) Phosphodiesterase (PDE) (2) PROTACs (1)
By Research Areas:	Cancer (21) Infection (2) Inflammation/Immunology (3)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156152A

CARM1 degrader-1 hydrochloride	Histone Methyltransferase PROTACs	Cancer
CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC₅₀ of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration .

HY-15214A

CARM1-IN-3 dihydrochloride	Histone Methyltransferase	Cancer
CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC₅₀ values of 0.07, >25 µM for CARM1 and CARM3, respectively .

HY-15214

CARM1-IN-3	Histone Methyltransferase	Cancer
CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC₅₀ values of 0.07, >25 µM for CARM1 and CARM3, respectively .

HY-158157

ZL-28-6	Histone Methyltransferase	Cancer
ZL-28-6 is a type I PRMT inhibitor (IC₅₀: 18 nM). ZL-28-6 effectively targets *CARM1* (a member of PRMT) within cells and can be used for cancer research .

HY-158158

CARM1-IN-5	Histone Methyltransferase	Cancer
CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of *CARM1* (IC₅₀= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines .

HY-161334

CARM1-IN-4	Histone Methyltransferase Apoptosis	Cancer
CARM1-IN-4 (compound 11f) is a potent *CARM1* inhibitor with IC₅₀s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .

HY-163561

CARM1-IN-6	Histone Methyltransferase	Cancer
CARM1-IN-6 (iCARM1) is an effective and selective inhibitor of *CARM1* with an IC₅₀ value of 12.3 μM. CARM1-IN-6 exhibits cell growth inhibitory activity and can be used in cancer research .

HY-156152

CARM1 degrader-1	Histone Methyltransferase	Cancer
PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC₅₀=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .

HY-156153

CARM1 degrader-2	Histone Methyltransferase	Cancer
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC₅₀=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .

HY-157388

CARM1/HDAC2-IN-1	Histone Methyltransferase HDAC	Cancer
CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against *CARM1* and HDAC2, with IC₅₀ values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity .

HY-12759A

CARM1-IN-1 hydrochloride 3 Publications Verification	Histone Methyltransferase	Cancer
CARM1-IN-1 hydrochloride is a potent and specific *CARM1* (Coactivator-associated arginine methyltransferase 1) inhibitor with IC₅₀ of 8.6 uM; shows very low activity against PRMT1 and SET7.

HY-12759

CARM1-IN-1 3 Publications Verification	Histone Methyltransferase	Cancer
CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).

HY-111109

EZM 2302 Maximum Cited Publications 8 Publications Verification	Histone Methyltransferase	Cancer
EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 6 nM.

HY-100855

DC_C66	Histone Methyltransferase	Cancer
DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC₅₀ of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC₅₀=21 μM), PRMT6 (IC₅₀= 47μM), and PRMT5 .

HY-117927

EPZ0025654 GSK3536023	Histone Methyltransferase	Cancer
EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 *CARM1), with IC₅₀* of 3 nM .

HY-100565

SGC2085 1 Publications Verification	Histone Methyltransferase	Cancer
SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC₅₀ value of 5.2 μM, but not other PRMT proteins .

HY-100565A

SGC2085 hydrochloride	Histone Methyltransferase	Cancer
SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC₅₀ value of 5.2 μM, but not other PRMT proteins .

HY-136809

PRMT6-IN-2	Others	Cancer
PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.

HY-114965

TP-064 5 Publications Verification	Histone Methyltransferase	Inflammation/Immunology Cancer
TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC₅₀ <10 nM). TP-064 inhibits dimethylation of BAF155 (IC₅₀ of 340 nM) and MED12 (IC₅₀ of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC₅₀ of 1.3 μM). TP-064 has anticancer activities .

HY-W013500

(1-Nitroethene-1,2-diyl)dibenzene alpha-Nitrostilbene; α-Nitrostilbene; NSC 385	Others	Others
(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC₅₀=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.

HY-110137A

Furamidine DB75; NSC 305831	Histone Methyltransferase Phosphodiesterase (PDE) Parasite	Infection Inflammation/Immunology Cancer
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .

HY-110137

Furamidine dihydrochloride 2 Publications Verification DB75 dihydrochloride; NSC 305831 dihydrochloride	Histone Methyltransferase Phosphodiesterase (PDE) Parasite	Infection Inflammation/Immunology Cancer
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .

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CARM1 inhibitor

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