Forvisirvat (SP-624) is an orally active, brain-penetrant and selective sirtuin 6 (SIRT6) activator. Forvisirvat activates the deacetylase activity of SIRT6, enhancing DNA repair and mitochondrial health, and exhibits antidepressant activity in animal models. Forvisirvat is promising for research of major depressive disorder.

PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research.

MPT0G413 (Compound 6) is a potent, selective, orally active and brain-penetrant HDAC6 inhibitor with an IC50 of 3.92 nM. MPT0G413 decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. MPT0G413 can ameliorate the impaired learning and memory. MPT0G413 can be used for the research of neurological disease, such as Alzheimer's disease.

SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer.

MC3935 is a LSD1 inhibitor with an IC50 of 0.52  μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.

ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms.

DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia.

LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.

LO-3-61, a JQ-1 analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.

ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer.

BTR2038 is a BRD9 degrader. BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function.

Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

UNC10415667 is a NSD2 degrader, with a DC50 values of 460 nM. UNC10415667 can be used for the study of cancers driven by NSD2 overexpression or dysregulation, such as multiple myeloma, acute lymphocytic leukemia, and prostate cancer.

CDD-1154 is an aminopyrimidine analog. CDD-1154 is a BRDT-BD2 inhibitor (IC50: 139 nM). CDD-1154 is used in male contraceptive research.

CDD-1498 (Compound 12) is a potent inhibitor of BRDT-BD2. CDD-1498 has an IC50 of 978 nM against BRDT-BD2. CDD-1498 can be studied in research on nonhormonal contraceptive agent.

CDD-1128 (Compound 11) is a potent inhibitor of BRDT-BD2. CDD-1128 has an IC50 of 521 nM against BRDT-BD2. CDD-1128 can be studied in research on nonhormonal contraceptive agent.

CDD-1147 is a BRDT-BD2 inhibitor with an IC50 of 94 nM. CDD-1147 can be used in the research of non-hormonal contraceptives for men.

CDD-1349 (Compound 15) is a BRDT-BD2/BRD4-BD2 selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC50 of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent.

CDD-1132 (Compound 8) is a potent inhibitor of BRDT-BD2. CDD-1132 has an IC50 of 13 nM against BRDT-BD2. CDD-1132 can be studied in research on nonhormonal contraceptive agent.

DCB29 is a selective inhibitor of the BPTF bromodomain, with an IC50 value of 13.2 μM. DCB29 can be used for the study of the treatment of BPTF-related diseases (such as bladder cancer, colorectal cancer, melanoma, leukemia, and other cancers).

Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

SKLB-11A is a selective, orally active and allosteric SIRT3 (sirtuin 3) agonist with a Kd value of 4.7 μM. SKLB-11A is highly selective for other members of the SIRT family. SKLB-11A activates autophagy-related signaling pathways, prevents mitochondrial dysfunction, improves cardiac function in Doxorubicin)-induced cardiotoxicity and myocardial ischemia/reperfusion models.

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research.

TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC50 of 5.1 nM and a Ki of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer.

Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).

SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).

MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research.

Z-MAL is a highly efficient and broad-spectrum HDAC substrate. Z-MAL exhibits high conversion activity for class I, II histone deacetylases, and class III SIRT1. Z-MAL can be used in studies on the structure-activity relationship, subtype selectivity, and inhibitor screening of HDAC.