| Cat. No. |
Product Name |
CAS No. |
Information |
| H9641 |
NSD1 inhibitor BT5
|
2351225-46-0 |
NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2;BT-5 displays liitle to no affinity against selected epigenetic enzymes, including 10 HDACs, 4 sirtuins and 6 HATs revealed no significant activity of BT5 at 50 uM.BT-5 demonstrates on-target activity in cells and blocks proliferation of NUP98-NSD1 cells with GI50 of 0.8-1.3 uM, human leukemia cell lines (K562, MOLM13 and SET2) with GI 50 of 6 uM.BT-5 inhibits NSD1 SET domain and impairs the activity of NUP98-NSD1 in leukemia cells, reduces the H3K36me2 level but not H3K36me3.BT-5 impairs colony formation in NUP98-NSD1 patient sample MLL-ENL translocation, reduces HOXA9 and MEIS1 expression, without cytotoxicity on normal CD34+ bone marrow progenitor cells. |
| H9590 |
Revumenib
|
2169919-21-3 |
Revumenib(SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM; SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). |
| H9256 |
Metoprine
|
7761-45-7 |
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT; Metoprine is an antifolate and antitumor agent |
| H9255 |
Furamidine
|
73819-26-8 |
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. |
| H9110 |
UNC926
|
1184136-10-4 |
UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM. |
| H9109 |
UNC926 hydrochloride
|
1184136-10-4 |
UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM. |
| H9018 |
menin-MLL inhibitor compound 2
|
2134674-44-3 |
menin-MLL inhibitor compound 2 is a potent menin-MLL inhibitor with IC50 value in the range of 250 nM to 1000 nM;useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. |
| H9017 |
KO-539
|
2134675-36-6 |
KO-539 is a novel, once-daily, oral investigational drug candidate targeting the menin-KMT2A/MLL protein-protein interaction for treatment of genetically defined AML patients with high unmet need; In preclinical models, KO-539 inhibits the KMT2A/MLL protein complex and has downstream effects on HOXA9/MEIS1 expression. KO-539 has received Orphan Drug Designation from the U.S. Food and Drug Administration for the treatment of AML. |
| H8854 |
Onametostat
|
2086772-26-9 |
Onametostat(JNJ-64619178)is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer. |
| H8679 |
MS1943
|
2225938-17-8 |
MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM; MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines. |
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