WM-1119
CAS 2055397-28-7
WM-1119 is a KAT6A/KAT6B inhibitor for epigenetic and cellular-senescence research. The primary study reports binding selectivity, lymphoma-cell growth inhibition and suppression of lymphoma progression in mice.
Epigenetics & Gene Regulation
Chromatin, transcription and epigenetic regulation.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
Epigenetics & Gene Regulation products
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ARV-771
CAS 1949837-12-0
ARV-771 is a VHL-recruiting BET protein degrader for prostate cancer and targeted protein degradation research. The primary study reports pan-BET degradation, downstream c-MYC suppression and activity in prostate cancer models.
WM-8014
CAS 2055397-18-5
WM-8014 is a KAT6A/KAT6B inhibitor for chromatin, cellular senescence and cancer research. Published work separates biochemical inhibition, fibroblast growth arrest and responses in a zebrafish liver cancer model.
MC3343
CAS 1535187-91-7
MC3343 is a nonnucleoside DNMT inhibitor for epigenetic reprogramming, osteoblastic differentiation and osteosarcoma research.
OTS193320
CAS 2093401-33-1
OTS193320 is a SUV39H2 methyltransferase inhibitor for histone methylation, DNA-damage-response and cancer-cell research.
OTS186935
CAS 2093400-18-9
OTS186935 is a SUV39H2 inhibitor with published cellular and xenograft activity, used in histone-methylation and cancer research.
SEC inhibitor KL-1
CAS 900308-84-1
KL-1 is a small-molecule disruptor of the super elongation complex for transcriptional elongation and MYC-dependent cancer research.
SEC inhibitor KL-2
CAS 900308-51-2
KL-2 is a small-molecule disruptor of the super elongation complex for transcriptional elongation and MYC-dependent cancer research.
STM2457
CAS 2499663-01-1
STM2457 is a catalytic METTL3 inhibitor for RNA methylation, leukemia-cell differentiation and cancer research.
PBIT
CAS 2514-30-9
PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1(JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1 ) histone demethylase an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC5 s of 6 and 4.9 μM, respectively[1].
Romidepsin（FK-228）
CAS 128517-07-7
Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s of 36 and 47 nM, respectively.
FLLL32
CAS 1226895-15-3
FLLL32 is a STAT3 inhibitor derived from the natural product curcumin. FLLL32 retains the cellular response to cytokines with anti-tumor activity[1].
DIM-C-pPhOCH3(C-DIM5)
CAS 33985-68-1
DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
CAY10603
CAS 1045792-66-2
CAY10603 is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
CDDO(Bardoxolone; RTA 401)
CAS 218600-44-3
Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
Bromosporine
CAS 1619994-69-2
Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2) [1]Target: BRD inhibitorIn cell-based…
UNC-1215
CAS 1415800-43-9
UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.
CPI203 (CPI-203)
CAS 1446144-04-2
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
CUDC-907 (PI3K/HDAC InhibitorI)
CAS 1339928-25-4
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
Nexturastat A
CAS 1403783-31-2
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.Nexturastat A displayed low micromolar activity compared to the low nanomolar activity against HDAC6. Moreover, it also demonstrated high levels of…
UNC-0638
CAS 1255580-76-7
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
BIX01294
CAS 935693-62-2
BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
OG-L002
CAS 1357302-64-7
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV…
RG108
CAS 48208-26-0
RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.
Rbin-1
CAS 328023-11-6
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136±7 nM.
Mivebresib(ABBV-075）
CAS 1445993-26-9
Mivebresib is a potent and orally available bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
Panobinostat(LBH589)
CAS 404950-80-7
Panobinostat is a non-selective histone deacetylase (HDAC) inhibitor.
MS436
CAS 1395084-25-9
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
S3I-201 (NSC-74859)
CAS 501919-59-1
NSC 74859 is a selective Stat3 inhibitor with an IC50 of 86±33 μM.
(S)-PFI-2 HCl
CAS 1627607-88-8
Negative control of (R)-PFI 2 hydrochloride. Exhibits 500-fold lower activity in a SETD7 enzymatic assay (IC50 = 1 μM) compared to the active enantiomer.
PFI-3
CAS 1819363-80-8
PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
UNC0321
CAS 1238673-32-9
UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.It was found that replacing the 5-carbon chain in compound 13 with an ethoxyethyl chain…
PTC-209 hydrobromide
CAS 1217022-63-3
PTC-209 hydrobromide is a specific BMI-1 inhibitor with IC50 of 0.5 μM in both GEMS reporter and ELISA assays.
UNC0379
CAS 1620401-82-2
UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.UNC0379 is a synthetic small-molecule inhibitor that displays inhibitory activity in multiple…
SGI-1027
CAS 1020149-73-8
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
Tranylcypromine HCl
CAS 1986-47-6
Tranylcypromine HCl is an inhibitor of monoamine oxidase (MAO) and prostacyclin synthase, potently suppresses the enzymatic activity of Lysine-Specific Demethylase 1 (LSD1) (IC50 <2 μM for BHC110/LSD1).
JIB-04
CAS 199596-05-9
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
PTC124 (Ataluren)
CAS 775304-57-9
Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
Belinostat (PXD101)
CAS 414864-00-9
Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780…
OF-1
CAS 919973-83-4
OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
BAY 87-2243
CAS 1227158-85-1
BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
EPZ011989
CAS 1598383-40-4
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646)Target: EZH2 inhibitorIn…
(+)-JQ1 PA
CAS 2115701-93-2
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
SIRT2 Inhibitor II, AK-7
CAS 420831-40-9
AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
SRPIN340
CAS 218156-96-8
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
UNC0631
CAS 1320288-19-4
UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM.UNC 0631, which had high in vitro potency versus G9a and improved lipophilicity, was highly potent (IC50 < 0.06 μM) in reducing H3K9me2 levels in MDA-MB-231 cells and had low cell toxicity. In…
wp1066（STAT Inhibitor III）
CAS 857064-38-1
WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
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