Search Result
Results for "
Anticancer
" in MCE Product Catalog:
1432
Inhibitors & Agonists
1
Biochemical Assay Reagents
44
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-115963
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Anticancer agent 38
|
Others
|
Cancer
|
Anticancer agent 38 (compound 19), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 38 inhibits A431 cell growth with an IC50 of 5.2 µg/mL.
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- HY-115962
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Anticancer agent 37
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Others
|
Cancer
|
Anticancer agent 37 (compound 18), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 37 inhibits HePG2 cell growth with an IC50 of 17.2 µg/mL.
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- HY-147968
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Anticancer agent 74
|
|
Cancer
|
Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell.
|
-
- HY-146396
-
Anticancer agent 51
|
Others
|
Cancer
|
Anticancer agent 51 (compound 3d) is a potent anticancer agent with an Ki of 731.62 nM. Anticancer agent 51 shows anticancer activity. Anticancer agent 51 has the potential for the research of prostate cancer.
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- HY-147971
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Anticancer agent 75
|
Parasite
Topoisomerase
|
Cancer
Infection
|
Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
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-
- HY-146030
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Anticancer agent 46
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Others
|
Cancer
|
Anticancer agent 46 (compound 2) is a potent anticancer agent. Anticancer agent 46 shows antiproliferative activity with an IC50 of 0.986 µM for MGC803 cells. Anticancer agent 46 has the potential for the research of gastric cancer.
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-
- HY-147906
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Anticancer agent 71
|
Apoptosis
PARP
|
Cancer
|
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity.
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-
- HY-147909
-
-
- HY-146063
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Anticancer agent 54
|
Apoptosis
|
Cancer
|
Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation.
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-
- HY-115960
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Anticancer agent 35
|
Others
|
Cancer
|
Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 35 inhibits A549, A431, PACA2 cell growth with IC50s of 18.1 µg/mL, 4.0 µg/mL, 18.9 µg/mL, respectively.
|
-
- HY-146407
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Anticancer agent 53
|
Apoptosis
|
Cancer
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity.
|
-
- HY-147918
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Anticancer agent 73
|
DNA/RNA Synthesis
|
Cancer
|
Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo.
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-
- HY-146433
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Anticancer agent 55
|
Apoptosis
|
Cancer
|
Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer.
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- HY-144808
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Anticancer agent 40
|
Others
|
Cancer
|
Anticancer agent 40 (compound 3e) is a potent anticancer agent. Anticancer agent 40 shows anticancer activities with IC50s of 0.94, 0.98, 0.96, 0.95, 2.13 nM for SKBR-3, SKOV-3, PC-3, U-87, HDF cells, respectively.
|
-
- HY-147816
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Anticancer agent 70
|
Mitochondrial Metabolism
|
Cancer
|
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential.
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- HY-146462
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Anticancer agent 59
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Apoptosis
ROS Kinase
|
Cancer
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model.
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- HY-146444
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Anticancer agent 56
|
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
|
Cancer
|
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with drug-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9.
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- HY-147514
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Anticancer agent 64
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
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- HY-115959
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Anticancer agent 34
|
Bacterial
|
Cancer
Inflammation/Immunology
|
Anticancer agent 34 (compound 9), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 34 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/ml. Anticancer agent 34 inhibits A549, PC3 cell growth with IC50s of 8.4 µg/ml, 7.8 µg/ml, respectively.
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- HY-115961
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Anticancer agent 36
|
Bacterial
|
Cancer
Inflammation/Immunology
|
Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively.
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- HY-146461
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Anticancer agent 58
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model.
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- HY-146452
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Anticancer agent 57
|
Apoptosis
|
Cancer
|
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC).
|
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- HY-147504
-
Anticancer agent 63
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity.
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- HY-146465
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Anticancer agent 60
|
Microtubule/Tubulin
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Cancer
|
Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model.
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- HY-146406
-
Anticancer agent 52
|
Apoptosis
|
Cancer
|
Anticancer agent 52 is a potent anticancer agent. Anticancer agent 52 shows in vitro cytotoxicity. Anticancer agent 52 induces apoptosis. Anticancer agent 52 shows antitumor effect. Anticancer agent 52 has the potential for the research of bladder cancer.
|
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- HY-146357
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Anticancer agent 48
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors.
|
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- HY-146358
-
Anticancer agent 49
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors.
|
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- HY-146286
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Anticancer agent 44
|
Apoptosis
|
Cancer
|
Anticancer agent 44 (compound 2a) is a potent anticancer agent. Anticancer agent 44 shows cytotoxicity activity in cancer cells. Anticancer agent 44 induces apoptosis. Anticancer agent 44 shows low toxicity towards activated lymphocytes of human blood.
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- HY-146548
-
-
- HY-146290
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Anticancer agent 45
|
Apoptosis
|
Cancer
|
Anticancer agent 46 (compound 2b) is a potent and selective anticancer agent. Anticancer agent 46 shows cytotoxicity activity in cancer cells. Anticancer agent 46 induces apoptosis. Anticancer agent 46 shows low toxicity towards activated lymphocytes of human blood.
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- HY-146040
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Anticancer agent 47
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Apoptosis
|
Cancer
|
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo.
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- HY-139711
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-
- HY-147782
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Anticancer agent 67
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Apoptosis
|
Cancer
|
Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog.
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- HY-147781
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Anticancer agent 66
|
Apoptosis
|
Cancer
|
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog.
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- HY-128689
-
-
- HY-78884
-
Anticancer agent 9
|
Others
|
Cancer
|
Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer.
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- HY-146516
-
Anticancer agent 42
|
MDM-2/p53
Apoptosis
ROS Kinase
|
Cancer
|
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer.
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- HY-147783
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Anticancer agent 68
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MDM-2/p53
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Cancer
|
Anticancer agent 68 is (Compound 12) is an anti-cancer agent. Anticancer agent 68 arrests the cells at the G2/M phase and induces programmed cell death. Anticancer agent 68 induces upregulation of tumor suppression via activation of p53 & PTEN.
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- HY-139635
-
-
- HY-146389
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Anticancer agent 50
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MDM-2/p53
P-glycoprotein
|
Cancer
|
Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
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- HY-146467
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Anticancer agent 62
|
Others
|
Cancer
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition.
|
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- HY-150571
-
-
- HY-146466
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Anticancer agent 61
|
Others
|
Cancer
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition.
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- HY-W072940
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-
- HY-146170
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Anticancer agent 69
|
Reactive Oxygen Species
EGFR
Apoptosis
|
Cancer
|
Anticancer agent 69 (Compound 34), a potent and selective anticancer agent , potently and selectively inhibits human prostate cancer cell line PC3 (IC50=26 nM). Anticancer agent 69 increases ROS level, down-regulates EGFR and induces apoptosis.
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- HY-141861
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Anticancer agent 17
|
Others
|
Cancer
|
Anticancer agent 17 displays potent anticancer activities against HeLa and A2780 cells with IC50 values of 0.19 μM and 0.09 μM, respectively.
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- HY-146511
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Anticancer agent 41
|
|
Cancer
|
Anticancer agent 41 is a potent anticancer agent, shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 3.99 μM.
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- HY-115947
-
Anticancer agent 33
|
Others
|
Cancer
|
Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM.
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- HY-115943
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Anticancer agent 30
|
CDK
|
Cancer
|
Anticancer agent 30 (compound 6f-Z), a 3-arylidene-2-oxindole derivative, is a selective CDK2 inhibitor with potent anticancer activity.
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- HY-115980
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Anticancer agent 39
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Apoptosis
|
Cancer
|
Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrial membrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM.
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- HY-146105
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Anticancer agent 65
|
Apoptosis
MDM-2/p53
ROS Kinase
MMP
Bcl-2 Family
|
Cancer
|
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells.
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- HY-144225
-
-
- HY-144227
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-
- HY-115942
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Anticancer agent 29
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CDK
|
Cancer
|
Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent, with IC50 values of 0.054 μM, 0.127 μM, 0.129 μM, 0.396 μM for CDK2, CDK1, CDK4 and CDK6, respectively.
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- HY-139705
-
-
- HY-143641
-
-
- HY-139860
-
-
- HY-139828
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Anticancer agent 14
|
Apoptosis
|
Cancer
|
Anticancer agent 14 is a lead compound (IC50: 0.20 to 0.65 μM) that induces apoptosis, cell cycle arrest, and loss of mitochondrial membrane potential in breast cancer cells.
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- HY-144232
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Anticancer agent 28
|
Others
|
Cancer
|
Anticancer agent 28 showed good antitumor activity in H22 allogeneic mice in vivo. Its potency in K562 cells was 50 times that of oridonin, and its < b > IC < sub > 50 < / sub > < / b > value was 0.09 μ M。
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- HY-139882
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Anticancer agent 16
|
Others
|
Cancer
|
Anticancer agent 16 exhibits good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively.
|
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- HY-147048
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STAT3 degrader-1
|
STAT
|
Cancer
|
STAT3 degrader-1 (compound 295) is a potent STAT3 degrader. STAT3 degrader-1 can be used for researching anticancer.
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- HY-146236
-
VEGFR-2-IN-27
|
VEGFR
|
Cancer
|
VEGFR-2-IN-27 (compound 7a) is a highly potent VEGFR-2 inhibitor with an IC50 value of 14.8 nM. VEGFR-2-IN-27 can be used for researching anticancer.
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- HY-147029
-
-
- HY-147218
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TAM&Met-IN-1
|
c-Met/HGFR
TAM Receptor
|
Cancer
|
TAM&Met-IN-1 is a potent TAM and c-Met kinase inhibitor with IC50 values of 6.1 nM, 13.2 nM and 21.6 nM for AXL, MER and TYRO3, respectively. TAM&Met-IN-1 can be used for researching anticancer.
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- HY-147031
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JAMM protein inhibitor 2
|
Others
|
Cancer
|
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2, respectively. JAMM protein inhibitor 2 can be used for researching anticancer
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-
- HY-146229
-
VEGFR-2-IN-25
|
VEGFR
|
Cancer
|
VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer.
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- HY-144965
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SOS1-IN-12
|
Ras
|
Cancer
|
SOS1-IN-12 is a potent son of sevenless homolog 1 (SOS1) inhibitor with a Ki of 0.11 nM for SOS1 and an IC50 of 47 nM for pERK. SOS1-IN-13 can be used for researching anticancer.
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- HY-143254
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Enpp-1-IN-10
|
Phosphodiesterase (PDE)
|
Cancer
|
Enpp-1-IN-10 (compound 1) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 3.866 μM. Enpp-1-IN-10 can be used for researching anticancer.
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- HY-147937
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AKT-IN-13
|
Akt
|
Cancer
|
AKT-IN-13 (compound 4b) is a potent Akt inhibitor with IC50s of 1.6 nM, 2.4 nM and 0.3 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-13 can be used for researching anticancer.
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-
- HY-144967
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SOS1-IN-13
|
Ras
|
Cancer
|
SOS1-IN-13 is a potent son of sevenless homolog 1 (SOS1) inhibitor with IC50s of 6.5 nM and 327 nM for SOS1 and pERK, respectively. SOS1-IN-13 can be used for researching anticancer.
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- HY-N8185
-
-
- HY-147282
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Amgen-23
|
SphK
|
Cancer
|
Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC50 values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer.
|
-
- HY-144333
-
-
- HY-146759
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ZM514
|
CD73
|
Cancer
|
ZM514 is a potent CD73 inhibitor with IC50s of 1.39 μM and 14.65 μM for hCD73 and mCD73, respectively. ZM514 has low cytotoxicity. ZM514 can be used for researching anticancer.
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- HY-144336
-
-
- HY-N0117
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Indirubin
Couroupitine B; Indigo red; Indigopurpurin
|
Apoptosis
|
Cancer
|
Indirubin (Couroupitine B) is a bis-indole alkaloid and has emarkable anticancer activity against chronic myelocytic leukemia.
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- HY-147649
-
Glyoxalase I inhibitor 7
|
Others
|
Cancer
|
Glyoxalase I inhibitor 7 (Compound 6) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 3.65 μM. Glyoxalase I inhibitor 7 can be used as anticancer agent.
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-
- HY-136554
-
WYC-210
|
Others
|
Cancer
|
WYC-210, a Tazarotene derivative, is a retinoid compound with lower anticancer activity.
|
-
- HY-145108
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FAK-IN-1
|
FAK
|
Cancer
|
FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)).
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- HY-146783
-
ZINC194100678
|
PAK
|
Cancer
|
ZINC194100678 is a potent PAK1 inhibitor with an IC50 value of 8.37 μM. ZINC194100678 can inhibit MDA-MB-231 cell proliferation. ZINC194100678 can be used for researching anticancer.
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-
- HY-147647
-
Glyoxalase I inhibitor 5
|
Others
|
Cancer
|
Glyoxalase I inhibitor 5 (Compound 9h) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.28 μM. Glyoxalase I inhibitor 5 can be used as anticancer agent.
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- HY-N7666
-
-
- HY-147648
-
Glyoxalase I inhibitor 6
|
Others
|
Cancer
|
Glyoxalase I inhibitor 6 (Compound 9j) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.13 μM. Glyoxalase I inhibitor 6 can be used as anticancer agent with low toxicity.
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- HY-130359
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Pericyclivine
|
Others
|
Cancer
|
Pericyclivine is a monomeric indole alkaloid isolated from Catharanthus Roseus. Pericyclivine has anticancer effects.
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-
- HY-136686
-
-
- HY-146566
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DNA-PK-IN-9
|
DNA-PK
|
Cancer
|
DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer.
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-
- HY-W008469
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2-Fluoroadenine
|
DNA/RNA Synthesis
|
Cancer
|
2-Fluoroadenine is a toxic purine bases. 2-Fluoroadenine has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for researching anticancer.
|
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- HY-145817
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(Rac)-RP-6306
|
Others
|
Cancer
|
(Rac)-RP-6306 (compound 181) is a potent Myt1 inhibitor with an IC50 of <10 nM. (Rac)-RP-6306 (compound 181) has anticancer effects.
|
-
- HY-N7809
-
-
- HY-147290
-
NSC 694623
|
Histone Acetyltransferase
|
Cancer
|
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer.
|
-
- HY-139986
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CDK7-IN-5
|
CDK
|
Cancer
|
CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104)).
|
-
- HY-137457A
-
Venadaparib hydrochloride
IDX-1197 hydrochloride
|
PARP
|
Cancer
|
Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research.
|
-
- HY-147526
-
RM-581
|
Others
|
Cancer
|
RM-581, an aminosteroid derivative, has potent anticancer activity in different types of cancer, including high fatality pancreatic cancer.
|
-
- HY-150614
-
-
- HY-144780
-
CXCR2 antagonist 4
|
CXCR
|
Cancer
|
CXCR2 antagonist 4 (compound 7) is a potent CXCR2 antagonist with an IC50 value of 0.13 μM. CXCR2 antagonist 4 can inhibit CXCL8-induced cytosolic calcium increase (IC50 = 27 μM). CXCR2 antagonist 4 can be used for researching anticancer.
|
-
- HY-N10444
-
-
- HY-143281
-
-
- HY-N6050
-
-
- HY-N7640
-
Deoxylimonin
|
Others
|
Cancer
Inflammation/Immunology
|
Desoxylimonin is a triterpenoid compound isolated from grapefruit seed. Desoxylimonin derivatives has better anticancer, analgesic and anti-inflammatory activitythan the lead compound.
|
-
- HY-150696
-
Antitumor agent-72
|
Apoptosis
Caspase
PARP
|
Cancer
|
Antitumor agent-72 (compound 6w) is a potent anticancer agent. Antitumor agent-72 has anticancer activity and induces apoptosis through activation of caspase-3 and cleavage of PARP. Antitumor agent-72 can be used for cancer research.
|
-
- HY-138558
-
-
- HY-N8187
-
Eupalinolide O
|
Apoptosis
|
Cancer
|
Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells.
|
-
- HY-13767
-
Tirapazamine
SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone
|
Others
|
Cancer
|
Tirapazamine is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.
Tirapazamine can enhance the cytotoxic effects of ionizing radiation in hypoxic cells.
|
-
- HY-138239
-
WEE1-IN-3
|
Wee1
|
Cancer
|
WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities.
|
-
- HY-137344
-
dAURK-4
|
Aurora Kinase
|
Cancer
|
dAURK-4, an Alisertib derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 has anticancer effects.
|
-
- HY-137344A
-
-
- HY-13670
-
Lurtotecan
GI147211; OSI-211
|
Topoisomerase
|
Cancer
|
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.
|
-
- HY-122096
-
DCLX069
|
Histone Methyltransferase
|
Cancer
|
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects.
|
-
- HY-14943
-
Darinaparsin
ZIO-101; S-Dimethylarsino-glutathione
|
Apoptosis
|
Cancer
|
Darinaparsin (ZIO-101), an organic arsenical, is a mitochondrial-targeted agent. Darinaparsin induces apoptosis in ancer cells, and has anticancer effects.
|
-
- HY-145664
-
Myt1-IN-1
|
Others
|
Cancer
|
Myt1-IN-1 is a potent Myt1 inhibitor with an IC50 of <10 nM. Myt1-IN-1 has anticancer effects (WO2021195782A1; compound 132).
|
-
- HY-145665
-
Myt1-IN-2
|
Others
|
Cancer
|
Myt1-IN-2 is a potent Myt1 inhibitor with an IC50 of <10 nM. Myt1-IN-2 has anticancer effects (WO2021195782A1; compound 28).
|
-
- HY-146092
-
-
- HY-147967
-
EGFR-IN-63
|
EGFR
|
Cancer
|
EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
|
-
- HY-W295873
-
Cyclo(Phe-Gly)
|
Bacterial
|
Cancer
Infection
|
Cyclo(Phe-Gly) is a cyclodipeptides with antimicrobial and anticancer activities, isolated from broth culture of endophytic Streptomyces YIM 64018 associated with Paraboea sinensis.
|
-
- HY-147136
-
MYF-03-176
|
Others
|
Cancer
|
MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration.
|
-
- HY-146335
-
CLK1/4-IN-1
|
CDK
|
Cancer
|
CLK1/4-IN-1 (compound 31) is a potent and selective Clk1 and Clk4 inhibitor with an IC50 value of 9.7 nM and 6.6 nM, respectively. CLK1/4-IN-1 has growth inhibitory activities against T24 cancer cells with GI50 of 1.1 μM. CLK1/4-IN-1 can be used for researching anticancer.
|
-
- HY-112130
-
AGI-24512
|
Others
|
Cancer
|
AGI-24512 is a methionine adenosyltransferase 2A (MATA2) inhibitor with an IC50 value of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.
|
-
- HY-147997
-
EGFR-IN-68
|
EGFR
|
Cancer
|
EGFR-IN-68 (Compound 8d) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-68 shows anticancer activity.
|
-
- HY-147996
-
EGFR-IN-67
|
EGFR
|
Cancer
|
EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity.
|
-
- HY-147995
-
EGFR-IN-64
|
EGFR
|
Cancer
|
EGFR-IN-64 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-64 shows anticancer activity.
|
-
- HY-135336
-
(R)-Verapamil hydrochloride
(R)-(+)-Verapamil hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
|
-
- HY-15865
-
FR901463
|
Others
|
Cancer
|
FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus.
|
-
- HY-117371
-
Hemiasterlin
(-)-Hemiasterlin; Milnamide B
|
ADC Cytotoxin
|
Cancer
|
Hemiasterlin ((-)-Hemiasterlin) is an antimitotic marine natural product with potent anticancer effcts. Hemiasterlin can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
|
-
- HY-N2965
-
-
- HY-132815
-
-
- HY-144337
-
DNA crosslinker 4 dihydrochloride
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer.
|
-
- HY-W031510
-
3,6-Dihydroxyxanthone
|
Others
|
Cancer
|
3,6-Dihydroxyxanthone (compound 3) is a xanthone derivatives. 3,6-Dihydroxyxanthone (compound 3) has anticancer activity. 3,6-Dihydroxyxanthone (compound 3) can be used for cancer research.
|
-
- HY-123396
-
8-Chloro-cAMP
|
PKA
|
Cancer
|
8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity.
|
-
- HY-147569
-
ATR-IN-17
|
ATM/ATR
|
Cancer
|
ATR-IN-17 (compound 88) is a potent ATR kinase inhibitor. ATR-IN-17 shows good anticancer activity in LoVo cells, with an IC50 of 1 nM.
|
-
- HY-137463
-
-
- HY-147568
-
ATR-IN-16
|
ATM/ATR
|
Cancer
|
ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor. ATR-IN-16 shows good anticancer activity in LoVo cells, with an IC50 of 410 nM.
|
-
- HY-137466
-
ARN-21934
|
Topoisomerase
|
Cancer
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
|
-
- HY-147601
-
CDK7-IN-16
|
CDK
|
Cancer
|
CDK7-IN-16 (compound 9) is a potent CDK 7 inhibitor with an IC50 range of 1 ~ 10 nM. CDK7-IN-16 can be used for researching anticancer, especially the cancer with transcriptional dysregulation.
|
-
- HY-146053
-
-
- HY-146065
-
FAK-IN-4
|
FAK
Apoptosis
|
Cancer
|
FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis.
|
-
- HY-N7985
-
Pendulone
|
Parasite
Bacterial
|
Cancer
Infection
|
Pendulone is a isoflavanquinone with good antiplasmodial activity with an IC50 of 7.0 µM. Pendulone also has antileishmanial, antibacterial and anticancer activity.
|
-
- HY-125938
-
Cycloartenyl ferulate
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Others
|
Cancer
Inflammation/Immunology
|
Cycloartenyl ferulate (Cycloartenol ferulate) is one of the typical triterpene alcohols and possesses several biological activities including anti-oxidative activity, antiallergic activity, anti-inflammatory and anticancer activities.
|
-
- HY-147291
-
VPC-70063
|
c-Myc
PARP
Apoptosis
|
Cancer
|
VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer.
|
-
- HY-146146
-
Kolavenic acid analog
KAA
|
Kinesin
|
Cancer
|
Kolavenic acid analog (KAA) is an anticancer agent. Kolavenic acid analog shows strong activity against HSET-overproducing yeast cells. Kolavenic acid analog inhibits centrosome clustering in human cancer cells containing high HSET levels and supernumerary centrosomes.
|
-
- HY-143255
-
Enpp-1-IN-11
|
Phosphodiesterase (PDE)
|
Cancer
|
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer.
|
-
- HY-131054
-
-
- HY-150567
-
SMO-IN-3
|
Smo
Hedgehog
|
Cancer
|
SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC50 value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.
|
-
- HY-150564
-
SMO-IN-2
|
Smo
Hedgehog
|
Cancer
|
SMO-IN-2 (compound 1) is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.
|
-
- HY-147941
-
MS9427
|
PROTACs
EGFR
|
Cancer
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
|
-
- HY-150619
-
KDM4-IN-4
|
Histone Demethylase
|
Cancer
|
KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer.
|
-
- HY-146390
-
Antiproliferative agent-5
|
Autophagy
Reactive Oxygen Species
|
Cancer
|
Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer.
|
-
- HY-147800
-
VEGFR-2-IN-21
|
VEGFR
|
Cancer
|
VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity.
|
-
- HY-116437
-
Selatinib
|
EGFR
|
Cancer
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
|
-
- HY-A0280
-
Roslin 2 bromide
Benzylhexamethylenetetramine bromide
|
MDM-2/p53
|
Cancer
|
Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator with anticancer effects. Roslin 2 bromide binds FAK, disrupts the binding of FAK and p53.
|
-
- HY-147780
-
Fissitungfine B
|
Others
|
Cancer
|
Fissitungfine B is a compound extracted from the tropical medicinal plant Fissistigma tungfangense. Fissitungfine B has strong anticancer activity.
|
-
- HY-146411
-
microRNA-21-IN-1
|
MicroRNA
Apoptosis
|
Cancer
|
microRNA-21-IN-1 (compound 7A) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer.
|
-
- HY-146287
-
Zn(BQTC)
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer.
|
-
- HY-134817
-
USP7-IN-8
|
Deubiquitinase
|
Cancer
|
USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
|
-
- HY-150572
-
CDK2-IN-11
|
CDK
Carbonic Anhydrase
|
Cancer
|
CDK2-IN-11 (compound 9d) is a potent CDK2 inhibitor with an IC50 of 6.4 μM, and KI values of 23.4 nM, 56.3 nM and 44.3 nM for hCA II, hCA IX and hCA XII, respectively. CDK2-IN-11 can be used for researching anticancer.
|
-
- HY-105846
-
Nogalamycin
|
DNA/RNA Synthesis
Bacterial
Antibiotic
|
Cancer
|
Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer.
|
-
- HY-122550
-
Artemisitene
|
Keap1-Nrf2
Topoisomerase
Apoptosis
|
Cancer
|
Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
|
-
- HY-145705
-
Pencitabine
|
DNA/RNA Synthesis
|
Cancer
|
Pencitabine (Pen) is an orally active anticancer agent. Pencitabine interferes with DNA synthesis and function by inhibiting multiple nucleotide-metabolizing enzymes and by misincorporation into DNA.
|
-
- HY-W012634
-
-
- HY-147926
-
VEGFR-2-IN-28
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity.
|
-
- HY-121002
-
-
- HY-132832
-
Sirpiglenastat
DRP-104
|
Others
|
Cancer
|
Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
|
-
- HY-144335
-
DNA crosslinker 2 dihydrochloride
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer.
|
-
- HY-145046
-
SOS1-IN-3
|
Ras
|
Cancer
|
SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1).
|
-
- HY-147231
-
SG3400 delate(Mal-amido-PEG8)
|
Others
|
Cancer
|
SG3400 delate (Mal-amido-PEG8) (compound 21) is an intermediate for the synthesis of ADC molecules. SG3400 delete is an effective toxin molecule with anticancer activity. SG3400 delete can be used in cancer research.
|
-
- HY-121410
-
-
- HY-149001
-
PARP1-IN-9
|
PARP
|
Cancer
|
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .
|
-
- HY-146786
-
ZMF-10
|
PAK
Apoptosis
|
Cancer
|
ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer.
|
-
- HY-B0077
-
Bendamustine hydrochloride
SDX-105
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-141482
-
WSB1 Degrader 1
|
E1/E2/E3 Enzyme
|
Cancer
|
WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.
|
-
- HY-122661
-
Mefuparib hydrochloride
MPH
|
PARP
Apoptosis
|
Cancer
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
|
-
- HY-147905
-
CDK9-IN-18
|
CDK
Apoptosis
|
Cancer
|
CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
|
-
- HY-16110
-
Tegafur-Uracil
UFT; BMS-200604
|
Others
|
Cancer
|
Tegafur-Uracil is an orally active fluoropyrimidines anticancer agent. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used for researching anti solid tumors.
|
-
- HY-N6794
-
10Z-Hymenialdisine
(Z)-Hymenialdisine; Hymenialdisine
|
AMPK
VEGFR
PDGFR
|
Cancer
|
10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.
|
-
- HY-121054
-
Chalcone
|
Bacterial
|
Cancer
Inflammation/Immunology
|
Chalcone is isolated from Glycyrrhizae inflata and used to synthesize chalcone derivatives. Chalcone derivatives possess varied biological and pharmacological activity, including anti-inflammatory, antioxidative, antibacterial, anticancer, and anti-parasitic activities.
|
-
- HY-147040
-
ABN401
|
c-Met/HGFR
|
Cancer
|
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer.
|
-
- HY-124651
-
SEMBL
|
NF-κB
MMP
|
Cancer
Inflammation/Immunology
|
SEMBL is a potent NF-κB inhibitor. SEMBL can inhibit NF-κB-DNA binding, and also inhibits NF-κB-dependent inflammatory cytokine secretions. SEMBL inhibits cancer cell migration and invasion via decreasing MMP expression. SEMBL can be used for researching anticancer.
|
-
- HY-13567
-
Bendamustine
SDX-105 free base
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-130331
-
Zaragozic acid B
|
Farnesyl Transferase
|
Cancer
|
Zaragozic acid B, a fungal metabolite, is a potent inhibitor of both farnesyl-protein transferase (FPTase) and squalene synthases. Zaragozic acid B is a potential anticancer drug.
|
-
- HY-144748
-
-
- HY-N8028
-
Quercetin 3-O-sambubioside
|
Others
|
Cancer
|
Quercetin-3-O-sambubioside is a monomeric compound found in Eucommia ulmoides male flowers. Quercetin-3-O-sambubioside promotes the stimulation of the nerve center. Antioxidant and anticancer activities.
|
-
- HY-147998
-
Enpp-1-IN-13
|
Phosphodiesterase (PDE)
|
Cancer
|
Enpp-1-IN-13 (Compound 1a) is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor with IC50 values of 1.29 μM and 20.2 μM against ENPP1 and ENPP3, respectively. Enpp-1-IN-13 shows anticancer activity.
|
-
- HY-116920
-
-
- HY-A0091
-
-
- HY-A0091A
-
-
- HY-15133
-
-
- HY-15866
-
FR901465
|
Others
|
Cancer
|
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research.
|
-
- HY-147799
-
hCA XII/II/IX-IN-1
|
Carbonic Anhydrase
|
Cancer
|
hCA XII/II/IX-IN-1 (Compound 3) is a potent human carbonic anhydrase (hCA) inhibitor with IC50 values of 2.6, 0.004, 0.005 and 0.001 μM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA XII/II/IX-IN-1 shows anticancer activity.
|
-
- HY-N1410
-
Triacetylresveratrol
|
STAT
NF-κB
|
Cancer
|
Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects.
|
-
- HY-N1438
-
Hydroxygenkwanin
7-O-Methylluteolin
|
Others
|
Cancer
|
Hydroxygenkwanin (7-O-Methylluteolin), a natural flavonoid compound, is one of the main components of Lilac Daphne. Hydroxygenkwanin has anti-oxidant ability, anti-glioma ability and anticancer effect.
|
-
- HY-32344
-
Inecalcitol
TX 522
|
VD/VDR
Apoptosis
|
Cancer
|
Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a Kd of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities.
|
-
- HY-13672
-
-
- HY-149027
-
Eleutherobin
|
Microtubule/Tubulin
|
Cancer
|
Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel. Anticancer activity.
|
-
- HY-105303
-
CEP-9722
|
PARP
|
Cancer
|
CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects.
|
-
- HY-15133A
-
-
- HY-146261
-
HI5
|
Microtubule/Tubulin
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.
|
-
- HY-103706
-
ROC-325
|
Autophagy
Apoptosis
|
Cancer
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
|
-
- HY-147066
-
Dyrk1A-IN-4
|
DYRK
|
Cancer
|
Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects.
|
-
- HY-124129
-
10074-A4
|
c-Myc
|
Cancer
|
10074-A4 is a c-Myc inhibitor. 10074-A4 could bind to c-Myc370-409 at different sites along the peptide chain. 10074-A4 has anticancer effects.
|
-
- HY-W010062
-
-
- HY-N10483
-
Telekin
|
Apoptosis
|
Cancer
|
Telekin is a eucalyptus-type sesquiterpene lactone compound found in the Chinese folk medicine Carpesium divaricatum. Telekin can activate mitochondria-mediated cell apoptosis and has anticancer activity.
|
-
- HY-19931
-
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-146459
-
Akt1-IN-1
|
Akt
|
Cancer
|
Akt1-IN-1 (compound 5b) is a potent and selective Akt1 inhibitor with an IC50 value of 18.79 nM in MIA Paca-2 cells. Akt1-IN-1 does not exhibit obvious teratogenicity, hepatotoxicity and cardiotoxicity (No Observed Adverse Effect Level > 100 µM). Akt1-IN-1 can be used for researching anticancer.
|
-
- HY-144870
-
STAT3-IN-7
|
STAT
|
Cancer
|
STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).
|
-
- HY-N8517
-
-
- HY-146999
-
-
- HY-N0872
-
-
- HY-119502
-
-
- HY-142922
-
BCR-ABL-IN-4
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
|
-
- HY-N2491
-
Deoxyelephantopin
|
NF-κB
|
Cancer
|
Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
|
-
- HY-120976
-
DEPMPO
|
Others
|
Cancer
|
cDEPMPO is a potent anticancer prodrug. High concentrations of DEPMPO spin-trap the ·OH radical together with aryl radicals arising from one-electron reduced BTO (benzotriazine 1,4-di-N-oxide) compounds.
|
-
- HY-19024
-
Merbarone
NSC 336628
|
Topoisomerase
|
Cancer
|
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
|
-
- HY-147204
-
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
|
Others
|
Cancer
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A).
|
-
- HY-N0247
-
Saikosaponin B1
|
Smo
|
Cancer
|
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO.
|
-
- HY-124962
-
D-NMAPPD
(1R,2R)-B13
|
Others
|
Cancer
Neurological Disease
|
D-NMAPPD ((1R,2R)-B13) is an acid ceramidase inhibitor. D-NMAPPD regulates NMDA receptor properties by enhancing endogenous production of ceramides. D-NMAPPD has anticancer effecs.
|
-
- HY-N9438
-
-
- HY-129566
-
-
- HY-146187
-
Antitumor agent-69
|
Histone Methyltransferase
|
Cancer
|
Antitumor agent-69 (compound 12) is a potent inhibitor of protein-protein interaction between DOT1L and MLL-AF9/MLL-ENL, with Kis of 9 nM and 109 nM for AF9 and ENL, respectively. Antitumor agent-69 exhibits anticancer cellular activitiy.
|
-
- HY-149033
-
Kobusine derivative-2
|
Others
|
Cancer
|
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity.
|
-
- HY-18061
-
Ochromycinone
(Rac)-STA-21
|
STAT
Bacterial
|
Cancer
Infection
|
Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
|
-
- HY-14397
-
Indomethacin
Indometacin
|
COX
|
Cancer
Inflammation/Immunology
|
Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research.
|
-
- HY-106588
-
Heptaplatin
SKI 2053R
|
Others
|
Cancer
|
Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles.
|
-
- HY-17423
-
Abacavir
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
Abacavir is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-143463
-
AC-386
|
c-Met/HGFR
|
Cancer
|
AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance.
|
-
- HY-138407
-
Evixapodlin
PD-1/PD-L1-IN 7
|
PD-1/PD-L1
HBV
|
Cancer
Infection
|
Evixapodlin (PD-1/PD-L1-IN 7) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC50 of 0.213 nM. Evixapodlin has anticancer and antiviral functions.
|
-
- HY-125924
-
DSPE-PEG(2000)-Amine
|
Others
|
Others
|
DSPE-PEG(2000)-Amine, an amine derivative of phospholipid poly ethylene glycol, is used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.
|
-
- HY-N7624
-
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
-
- HY-124629
-
DB2313
|
Apoptosis
|
Cancer
|
DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects.
|
-
- HY-14397A
-
Indomethacin sodium hydrate
Indometacin sodium hydrate
|
COX
Bacterial
Influenza Virus
|
Cancer
Inflammation/Immunology
|
Indomethacin (Indometacin) sodium hydrateis a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium hydrateis has anticancer activity and anti-infective activity. Indomethacin sodium hydrateis can be used for cancer, inflammation and viral infection research.
|
-
- HY-134823
-
MD-222
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
|
-
- HY-147838
-
Nampt-IN-9
|
NAMPT
|
Cancer
|
Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research.
|
-
- HY-14645
-
(-)-DHMEQ
Dehydroxymethylepoxyquinomicin
|
NF-κB
|
Cancer
Inflammation/Immunology
|
(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.
|
-
- HY-N0656
-
Usnic acid
|
Bacterial
|
Cancer
Infection
|
Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1.
|
-
- HY-N2307A
-
Lirinidine
(+)-Lirinidine
|
Others
|
Cancer
|
Lirinidine ((+)-Lirinidine) is an alkaloid isolated from the leaves of L. tulipifera and has antioxidant and anticancer activities. Lirinidine exhibits medium ferric reducing power activity and minor radical scavenging activity in vitro. Lirinidine can be used for cosmetic research.
|
-
- HY-121362
-
-
- HY-146367
-
-
- HY-10088
-
Zibotentan
ZD4054
|
Endothelin Receptor
Apoptosis
|
Cancer
Endocrinology
|
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
|
-
- HY-147566
-
ATR-IN-14
|
ATM/ATR
|
Cancer
|
ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC50 of 64 nM.
|
-
- HY-147991
-
-
- HY-N9507
-
Picrasidine Q
|
Apoptosis
FGFR
|
Cancer
|
Picrasidine Q, an alkaloid component extracted from Angelica keiskei species, has the capacity of anti-cell transformation and anti-cancer. Picrasidine Q induces cell apoptosis and G1 phase arrest in human esophageal cancer cell lines, and directly inhibits FGFR2 kinase activity.
|
-
- HY-146008
-
hCAII-IN-3
|
Carbonic Anhydrase
|
Cancer
|
hCAII-IN-3 (Compound 16) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 403.8, 5.1, 10.2 and 5.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-2 shows anticancer activity.
|
-
- HY-17423B
-
Abacavir monosulfate
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Cancer
Infection
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-126856
-
HC-Toxin
|
HDAC
Apoptosis
|
Cancer
|
HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.
|
-
- HY-150500
-
HDAC-IN-44
|
HDAC
|
Cancer
|
HDAC-IN-44 is a HDAC inhibitor with the IC50 value of 61.2 nM. HDAC-IN-44 shows high anticancer activity towards multiple cancer cell lines.
|
-
- HY-145303
-
-
- HY-108547
-
Alexidine dihydrochloride
|
Fungal
Apoptosis
|
Infection
|
Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens.
|
-
- HY-146420
-
GRP78-IN-2
|
HSP
|
Cancer
Cardiovascular Disease
|
GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells.
|
-
- HY-146007
-
hCA IX-IN-1
|
Carbonic Anhydrase
|
Cancer
|
hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 331.4, 28.4, 9.4 and 17.8 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-1 shows anticancer activity.
|
-
- HY-17423A
-
Abacavir sulfate
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
|
-
- HY-N7523
-
Neoxanthin
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions.
|
-
- HY-N0068
-
-
- HY-146274
-
c-Met-IN-10
|
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer.
|
-
- HY-15198
-
KG5
|
Raf
PDGFR
FLT3
c-Kit
|
Cancer
|
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
|
-
- HY-10515
-
BX-320
|
PDK-1
|
Cancer
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
|
-
- HY-100711
-
-
- HY-14518
-
Aminopterin
4-Aminofolic acid; APGA
|
Antifolate
|
Cancer
Inflammation/Immunology
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.
|
-
- HY-W018326
-
Temozolomide acid
|
DNA/RNA Synthesis
|
Cancer
|
Temozolomide acid is a carboxylic acid derivative of Temozolomide. Temozolomide is a DNA alkylating agent, methylating the guanine and adenine bases of DNA, causing breaks in DNA double strand, cell cycle arrest, and eventually cell death. Temozolomide acid has an activity similar to the parent compound Temozolomide with the same anticancer activity.
|
-
- HY-N10354
-
27-Methyl withaferin A
|
Apoptosis
|
Cancer
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively.
|
-
- HY-147786
-
TGFβRI-IN-5
|
TGF-β Receptor
|
Cancer
|
TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference drug against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.
|
-
- HY-149030
-
DHODH-IN-21
|
Dihydroorotate Dehydrogenase
|
Cancer
|
DHODH-IN-21 (compound 19) is a selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 1.1 nM. DHODH-IN-21 has anticancer activity and can be used in studies of acute myeloid leukaemia (AML).
|
-
- HY-15994
-
Citarinostat
ACY241
|
HDAC
|
Cancer
|
Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects.
|
-
- HY-100711A
-
-
- HY-120290
-
PU141
|
Histone Acetyltransferase
|
Cancer
|
PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
|
-
- HY-115975
-
GRPR antagonist-2
|
Others
|
Cancer
|
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.
|
-
- HY-N7113
-
Squalane
|
Others
|
Cancer
|
Squalane, found in certain fish oils (especially shark liver oil), and some vegetable oils, is a saturated derivative of Squalene. Squalane shows anticancer, antioxidant, skin hydrating, and emollient activities.
|
-
- HY-139297
-
SCR130
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity.
|
-
- HY-144299
-
-
- HY-143253
-
Estrogen receptor antagonist 7
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities.
|
-
- HY-145969
-
β-S-ARCA
|
Others
|
Others
|
β-S-ARCA is a mRNA 7-methylguanosine (m 7G) cap analog carrying a phosphorothioate (PS) moiety. mRNAs incorporating β-S-ARCA have elongated cellular half-lives and showed augmented protein expression. β-S-ARCA D1 has been applied in researching experimental mRNA-based anticancer vaccines.
|
-
- HY-108444
-
(Z)-FeCP-oxindole
|
VEGFR
|
Cancer
|
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 220 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM.
|
-
- HY-147413
-
Unecritinib
TQ-B3101
|
EGFR
|
Cancer
|
Unecritinib (TQ-B3101) is a potent EGFR tyrosine kinase inhibitor. Unecritinib shows anticancer activity. Unecritinib inhibits ALK, ROS1, and MET. Unecritinib has the potential for the research of solid tumor and relapsed or refractory ALK-positive anaplastic large cell lymphoma.
|
-
- HY-139324
-
Cu(II)GTSM
|
GSK-3
Amyloid-β
|
Neurological Disease
|
Cu(II)GTSM, a cell-permeable Cu-complex, significantly inhibits GSK3β. Cu(II)GTSM inhibits Amyloid-β oligomers (AβOs) and decreases tau phosphorylation. Cu(II)GTSM also decreases the abundance of Amyloid-β trimers. Cu(II)GTSM is a potential anticancer and antimicrobial agent.
|
-
- HY-136658
-
-
- HY-13540
-
E7016
GPI 21016
|
PARP
|
Cancer
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
|
-
- HY-N10411
-
-
- HY-Y0445A
-
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-100504
-
S-methyl DM1
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects.
|
-
- HY-114965
-
TP-064
|
Histone Methyltransferase
|
Cancer
Inflammation/Immunology
|
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-119974
-
Caracemide
NSC-253272
|
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide is a novel anticancer agent derived from a hydroxamic acid and has demonstrated to produce severe central nervous system (CNS) toxicity.
|
-
- HY-10082A
-
(E)-3-AP
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
|
DNA/RNA Synthesis
|
Cancer
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis.
|
-
- HY-15290
-
AIM-100
|
Ack1
|
Cancer
|
AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.
|
-
- HY-146169
-
Antitumor agent-68
|
Reactive Oxygen Species
Microtubule/Tubulin
|
Cancer
|
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 µM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner.
|
-
- HY-19747
-
HPOB
|
HDAC
Apoptosis
|
Cancer
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
|
-
- HY-106338
-
Polyketomycin
|
Bacterial
ADC Cytotoxin
Parasite
|
Cancer
Infection
|
Polyketomycin is a tetracyclic quinone glycoside antibiotic isolated from Streptomyces sp. or Streptomyces diastatochromogenes. Polyketomycin inhibits growth of Gram-positive bacteria, and its MIC values is less than 0.2 µg/mL. Polyketomycin has antibacterial, anticancer, antimalarial activities.
|
-
- HY-136657
-
SC-43
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
|
-
- HY-150655
-
Hsp90-IN-15
|
HSP
|
Cancer
|
Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell.
|
-
- HY-16576A
-
(Z)-SMI-4a
|
Pim
|
Cancer
|
(Z)-SMI-4a is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 µM. (Z)-SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. (Z)-SMI-4a has anticancer activity.
|
-
- HY-146160
-
PARP-1/HDAC-IN-1
|
PARP
HDAC
|
Cancer
|
PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities.
|
-
- HY-N2454
-
-
- HY-137371
-
-
- HY-119500
-
-
- HY-114489B
-
-
- HY-114489A
-
Haemanthamine
|
Apoptosis
Influenza Virus
Parasite
|
Cancer
Infection
Neurological Disease
|
Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
|
-
- HY-132193
-
RET-IN-4
|
RET
|
Cancer
|
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
|
-
- HY-N5033
-
17-Hydroxy sprengerinin C
|
Others
|
Cancer
|
17-Hydroxy sprengerinin C (compound 10) is a glycoside compound isolated from rhizomes of Polygonatum sibiricum. 17-Hydroxy sprengerinin C possesses stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.
|
-
- HY-119109
-
Laminaran
|
Others
|
Cancer
|
Laminaran is an β-1-3-glucan and a typical ligand for Dectin-1 from Eisenia Bicyclis, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
|
-
- HY-N0063
-
Punicalagin
|
SARS-CoV
HBV
|
Cancer
Infection
Metabolic Disease
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19.
|
-
- HY-139342
-
CDK7-IN-4
LY3405105
|
CDK
|
Cancer
|
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner.
|
-
- HY-13622
-
Elomotecan hydrochloride
BN 80927
|
Topoisomerase
|
Cancer
|
Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II.
|
-
- HY-146013
-
Sirt1/2-IN-1
|
Sirtuin
Microtubule/Tubulin
|
Cancer
|
Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity.
|
-
- HY-P99111
-
Golimumab
CNTO-148
|
TNF Receptor
Apoptosis
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research.
|
-
- HY-150761
-
MY-875
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.
|
-
- HY-147039
-
BOLD-100
|
HSP
Autophagy
|
Cancer
|
BOLD-100 is a ruthenium-based anticancer agent. BOLD-100 also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution.
|
-
- HY-N0104
-
Curcumol
(-)-Curcumol
|
Apoptosis
|
Cancer
|
Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
|
-
- HY-N6642
-
Ankaflavin
|
PPAR
Apoptosis
|
Cancer
Inflammation/Immunology
|
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects.
|
-
- HY-128756
-
SIAIS178
|
PROTACs
Bcr-Abl
|
Cancer
|
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
|
-
- HY-B1474
-
Alexidine
|
Fungal
|
Infection
Cancer
|
Alexidine, a bis-biguanide, exhibits antifungal and antibiofilm activity against a diverse range of fungal pathogens. Alexidine is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis.
|
-
- HY-150511
-
3-(3-Phenoxybenzyl)amino-β-carboline
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity.
|
-
- HY-146710
-
RET-IN-16
|
RET
|
Cancer
|
RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects.
|
-
- HY-143403
-
PI3K-IN-31
|
PI3K
|
Cancer
|
PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects.
|
-
- HY-147911
-
COX-2/PI3K-IN-1
|
PI3K
COX
|
Cancer
Inflammation/Immunology
|
COX-2/PI3K-IN-1 (compound 5d) is a potent PI3K inhibitor with IC50 value of 1.14 nM. COX-2/PI3K-IN-1 is a selective COX-2 inhibitor with Ki value of 3.24 nM. COX-2/PI3K-IN-1 has anti-inflammatory and anti-cancer properties.
|
-
- HY-116147
-
Ceranib-2
|
LPL Receptor
Apoptosis
|
Cancer
|
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.
|
-
- HY-125911
-
Gossypin
|
NF-κB
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Gossypin is a flavone isolated from Hibiscus vitifolius and has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits RANKL-induced osteoclastogenesis both in mouse primary bone marrow cells and RAW 264.7 cells in vitro.
|
-
- HY-W062835
-
CGP77675
|
Src
|
Cancer
|
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.
|
-
- HY-129388A
-
Pulrodemstat
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-N0036
-
Costunolide
(+)-Costunolide; Costus lactone
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells.
|
-
- HY-N2369
-
Chelidonine
|
Apoptosis
Influenza Virus
|
Cancer
Infection
|
Chelidonine is an isoquinoline alkaloid, can be isolated from Chelidonium majus L.. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanoma cell lines. with anticancer and antiviral activity.
|
-
- HY-135775
-
BMVC
|
G-quadruplex
Telomerase
DNA/RNA Synthesis
|
Cancer
|
BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.
|
-
- HY-110150
-
UNC3230
|
Others
|
Cancer
Inflammation/Immunology
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
|
-
- HY-147912
-
COX-2/PI3K-IN-2
|
PI3K
COX
|
Cancer
Inflammation/Immunology
|
COX-2/PI3K-IN-2 (compound 5f) is a potent PI3K inhibitor with IC50 value of 2.78 nM. COX-2/PI3K-IN-2 is a selective COX-2 inhibitor with Ki value of 3.02 nM. COX-2/PI3K-IN-2 shows anti-inflammatory and anti-cancer properties.
|
-
- HY-142685
-
Pyruvate Carboxylase-IN-2
|
Others
|
Cancer
|
Pyruvate Carboxylase-IN-2 (compound 29) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.065 and 0.097 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-2 is a natural analog of erianin. Pyruvate Carboxylase-IN-2 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC).
|
-
- HY-142684
-
Pyruvate Carboxylase-IN-1
|
Others
|
Cancer
|
Pyruvate Carboxylase-IN-1 (compound 37) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.204 and 0.104 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-1 is a natural analog of erianin. Pyruvate Carboxylase-IN-1 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC).
|
-
- HY-138280
-
DTHIB
|
HSP
|
Cancer
|
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.
|
-
- HY-128153
-
Thienopyridone
|
Phosphatase
Apoptosis
|
Cancer
|
Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects.
|
-
- HY-N7363
-
Isolongifolene
(-)-Isolongifolene
|
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of PI3K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
|
-
- HY-131031
-
KCC-07
|
DNA Alkylator/Crosslinker
|
Cancer
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
|
-
- HY-W062835A
-
CGP77675 hydrate
|
Src
|
Cancer
|
CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.
|
-
- HY-129388B
-
Pulrodemstat benzenesulfonate
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-15128
-
-
- HY-143462
-
c-Met/HDAC-IN-2
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance.
|
-
- HY-142956
-
ROS-ERS inducer 1
|
Others
|
Cancer
|
ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin.
|
-
- HY-145432
-
PI3K-IN-28
|
PI3K
|
Cancer
|
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents.
|
-
- HY-115528
-
-
- HY-113914
-
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-110078
-
Eeyarestatin I
|
p97
Apoptosis
|
Cancer
|
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
|
-
- HY-143905
-
PROTAC TTK degrader-2
|
PROTACs
|
Cancer
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
|
-
- HY-143904
-
PROTAC TTK degrader-1
|
PROTACs
|
Cancer
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
|
-
- HY-147224
-
OBX02-011
|
EGFR
|
Cancer
|
OBX02-011 is a potent and reversible fourth-generation EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor. OBX02-011 shows potent anticancer effects and inhibits EGFR-related signaling. OBX02-011 overcomes C797S-mediated resistance in NSCLC (non-small cell lung cancer).
|
-
- HY-129388
-
Pulrodemstat Methylbenzenesulfonate
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-147056
-
PKRA83
PKRA7
|
Others
|
Cancer
|
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.
|
-
- HY-133108
-
-
- HY-125817
-
BI-3406
|
Ras
p38 MAPK
|
Cancer
|
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
|
-
- HY-129476
-
L-Canaline
|
Parasite
Endogenous Metabolite
|
Cancer
Infection
|
L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects.
|
-
- HY-B0444A
-
Maprotiline
|
Autophagy
|
Cancer
Neurological Disease
|
Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect.
|
-
- HY-17514
-
Itraconazole
R51211
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
|
-
- HY-115974
-
GRPR antagonist-1
|
Others
|
Cancer
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.
|
-
- HY-13518
-
Piceatannol
Astringenin; trans-Piceatannol
|
Syk
Autophagy
Apoptosis
|
Cancer
|
Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI). Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. Piceatannol induces apoptosis in DLBCL cell lines. Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells.
|
-
- HY-124953
-
7,3',4'-Trihydroxyisoflavone
|
MAP3K
Apoptosis
|
Cancer
|
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities.
|
-
- HY-147892
-
HDAC-IN-42
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase.
|
-
- HY-107412
-
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-119374
-
BRM/BRG1 ATP Inhibitor-1
|
Epigenetic Reader Domain
|
Cancer
|
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity[1] .
|
-
- HY-N0279
-
-
- HY-115907
-
K20
|
Ras
Apoptosis
|
Cancer
|
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity.
|
-
- HY-125918
-
Bleomycin A5 hydrochloride
Pingyangmycin hydrochloride
|
Apoptosis
Antibiotic
|
Cancer
Infection
|
Bleomycin A5 (Pingyangmycin) hydrochloride is an anti-neoplastic glycoprotein antibiotic. Bleomycin A5 suppresses Drp1-mediated mitochondrial fission and induces apoptosis in human nasal polyp-derived fibroblasts. Bleomycin A5 hydrochloride has anticancer activities relying on its ability to produce RNA and DNA breaks, thus, leading to cell death..
|
-
- HY-N1029
-
Norathyriol
Mangiferitin
|
Glucosidase
PPAR
|
Cancer
Infection
Inflammation/Immunology
|
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
|
-
- HY-107146
-
PZ-128
P1pal-7
|
Protease Activated Receptor (PAR)
|
Cancer
Cardiovascular Disease
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
|
-
- HY-150748
-
ODN D-SL01
|
Toll-like Receptor (TLR)
|
Cancer
Inflammation/Immunology
|
ODN D-SL01, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 has strong immunostimulatory activity in a variety of vertebrate species and has anticancer activity. ODN D-SL01 sequence: 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'.
|
-
- HY-124526
-
Chiauranib
CS2164
|
VEGFR
PDGFR
c-Kit
Aurora Kinase
c-Fms
|
Cancer
|
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.
|
-
- HY-18979
-
Lactimidomycin
|
Influenza Virus
|
Cancer
Infection
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
|
-
- HY-16050
-
Plitidepsin
Aplidine
|
DNA/RNA Synthesis
SARS-CoV
|
Cancer
Infection
|
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM). Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.
|
-
- HY-144636
-
Atg4B-IN-2
|
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer drugs via autophagy inhibition.
|
-
- HY-115903
-
HIF-1α-IN-2
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
|
-
- HY-12354
-
SB-3CT
|
MMP
|
Cancer
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity.
|
-
- HY-135954A
-
PDK4-IN-1 hydrochloride
|
PDHK
Apoptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
|
-
- HY-122903
-
TK216
|
DNA/RNA Synthesis
|
Cancer
|
TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
|
-
- HY-135954
-
PDK4-IN-1
|
PDHK
Apoptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
|
-
- HY-126052
-
Gnetol
|
COX
Tyrosinase
HDAC
|
Cancer
Metabolic Disease
|
Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
|
-
- HY-D0190
-
2-Thenoyltrifluoroacetone
HTTA; TTA; TTFA
|
Others
|
Cancer
Infection
Others
|
2-Thenoyltrifluoroacetone is a chelating agent. 2-Thenoyltrifluoroacetone can be used for the complexation of various metal ions including Mn(II), Co(III), Ni(II), et al.. 2-Thenoyltrifluoroacetone possesses antitubercular and cytotoxic activities. 2-Thenoyltrifluoroacetone is also used as common inhibitor of mitochondrial electron flux and to analyze the endothelial cell dysfunction. Besides, copper (II) complex of 2-Thenoyltrifluoroacetone has anticancer activity against K562.
|
-
- HY-135318
-
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-107845
-
SCR7 pyrazine
|
CRISPR/Cas9
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
|
-
- HY-147891
-
Angiogenesis inhibitor 3
|
Apoptosis
|
Cancer
|
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos.
|
-
- HY-147890
-
Angiogenesis inhibitor 2
|
Apoptosis
|
Cancer
|
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos.
|
-
- HY-146087
-
Autophagy inducer 4
|
Autophagy
|
Cancer
|
Autophagy inducer 4 is a Magnolol-based Mannich base derivatives, which can be used as an anticancer agent. Autophagy inducer 4 suppresses cancer cells via inducing autophagy. Autophagy inducer 4 has 76-fold improvement in cytotoxicity against T47D cells compared with Magnolol. Autophagy inducer 4 also possesses suppressive effects on migration of T47D and Hela cancer cells.
|
-
- HY-125027
-
Isobutyl-deoxynyboquinone
IB-DNQ
|
Others
|
Cancer
|
Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1). Isobutyl-deoxynyboquinone can be used for the research of anticancer.
|
-
- HY-133124
-
PARP/PI3K-IN-1
|
PARP
PI3K
Apoptosis
|
Cancer
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
|
-
- HY-111373
-
RapaLink-1
|
mTOR
Autophagy
|
Cancer
|
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
|
-
- HY-19357
-
E3330
APX-3330
|
DNA/RNA Synthesis
|
Cancer
|
E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.
|
-
- HY-147822
-
Apoptosis inducer 6
|
Apoptosis
|
Cancer
|
Apoptosis inducer 6 (compound 4e) is an anticancer agent with a broad-spectrum anticancer activity. Apoptosis inducer 6 triggers cell death through the induction of apoptosis.
|
-
- HY-13733
-
-
- HY-N0010
-
-
- HY-N0293
-
Paeoniflorin
Peoniflorin
|
HSP
|
Cancer
Infection
Neurological Disease
|
Paeoniflorin is a heat shock protein-inducing compound and commonly exists in the plants of Paeoniaceae family, with various biological activities, including anticancer activity, anti-inflammatory activity, enhancing cognition and attenuating learning impairment, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, and reducing blood viscosity.
|
-
- HY-147696
-
SMTIN-T140
|
HSP
AMPK
Reactive Oxygen Species
|
Cancer
|
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells.
|
-
- HY-13770
-
-
- HY-12742
-
SCR7
|
DNA/RNA Synthesis
CRISPR/Cas9
Apoptosis
|
Cancer
|
SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
|
-
- HY-147864
-
c-Fms-IN-12
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.
|
-
- HY-N0053
-
Psoralen
Ficusin
|
Apoptosis
HIV
Influenza Virus
|
Cancer
|
Psoralen (Ficusin) is a coumarin isolated from the seeds of Fructus Psoraleae. Psoralen exhibits a wide range of biological properties, including anti-cancer, antioxidant, antidepressant, anticancer, antibacterial, and antiviral, et al.
|
-
- HY-147697
-
-
- HY-12352A
-
HJC0416 hydrochloride
|
STAT
Apoptosis
|
Cancer
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.
|
-
- HY-N0560
-
-
- HY-N8199
-
-
- HY-N7669
-
-
- HY-N0819
-
Raddeanin A
|
Apoptosis
|
Cancer
|
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
|
-
- HY-123114
-
-
- HY-18973
-
-
- HY-N7670
-
-
- HY-15385
-
Imexon
BM 06002
|
Others
|
Cancer
|
Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.
|
-
- HY-15044
-
NU1025
|
PARP
|
Cancer
Neurological Disease
|
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity.
|
-
- HY-123295
-
HDAC3-IN-T247
|
HDAC
|
Cancer
Infection
|
HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells.
|
-
- HY-N0540
-
Cynaroside
Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside
|
Influenza Virus
DNA/RNA Synthesis
Apoptosis
Parasite
Bacterial
Fungal
|
Cancer
Infection
|
Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities.
|
-
- HY-150582
-
c-Met-IN-14
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.
|
-
- HY-146682
-
KS100
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase.
|
-
- HY-N0796
-
-
- HY-B2102
-
Oxyphenisatine
Oxyphenisatin
|
Others
|
Cancer
|
Oxyphenisatine (Oxyphenisatin) is a laxative. Oxyphenisatin acetate is the pro-drug of oxyphenisatin with anticancer activity.
|
-
- HY-14812
-
-
- HY-N0725
-
-
- HY-16777
-
-
- HY-133097
-
-
- HY-106178
-
PMX-53
3D53
|
Complement System
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
|
-
- HY-146683
-
KS106
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase.
|
-
- HY-145260
-
BRD4/CK2-IN-1
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-120720
-
-
- HY-16941
-
-
- HY-15167
-
-
- HY-W012313
-
-
- HY-N10346
-
-
- HY-N0566
-
-
- HY-N0453
-
-
- HY-115952
-
-
- HY-147631
-
-
- HY-147133
-
VEGFR2-IN-2
|
VEGFR
|
Cancer
|
VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
|
-
- HY-147164
-
-
- HY-N6898
-
-
- HY-N0236
-
-
- HY-P1539
-
-
- HY-N0521A
-
-
- HY-W011311
-
-
- HY-126066
-
-
- HY-N6087
-
-
- HY-N7636
-
-
- HY-N9225
-
-
- HY-122930
-
-
- HY-N8346
-
-
- HY-N0007
-
-
- HY-N0669
-
Stevioside
|
Others
|
Cancer
|
Stevioside is a natural sweetener extracted from leaves of Stevia rebaudiana, with anticancer activity.
|
-
- HY-N9451
-
-
- HY-N8995
-
Bruceoside A
|
Others
|
Cancer
|
Bruceoside A, an abundant quassinoid glycoside in Fructus Bruceae, possesses anti-cancer activity.
|
-
- HY-N0902
-
Dihydrosanguinarine
13,14-Dihydrosanguinarine
|
Fungal
|
Infection
|
Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.
|
-
- HY-112440
-
-
- HY-N0182
-
-
- HY-N4259
-
-
- HY-116518
-
-
- HY-13741
-
RH1
NSC 697726
|
Others
|
Cancer
|
RH1 (NSC 697726) is a potent bioreductive agent with profound anti-cancer activity in vitro and in vivo.
|
-
- HY-N1247
-
Scabertopin
|
Others
|
Cancer
|
Scabertopin is a sesquiterpene lactone. Scabertopin has been found to be prominent anticancer constituents.
|
-
- HY-N4087
-
-
- HY-103128
-
-
- HY-N0280
-
Corosolic acid
Colosolic acid
|
Autophagy
|
Cancer
|
Corosolic acid (Colosolic acid) isolated from the fruit of Cratoegus pinnatifida var. psilosa, was reported to have anticancer activity.
|
-
- HY-N2052
-
-
- HY-N5052
-
-
- HY-16212
-
FR901464
|
Others
|
Cancer
|
FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects.
|
-
- HY-111761
-
DIQ3
|
Others
|
Cancer
|
DIQ3 is a potent anti-cancer agent, nontoxic to normal human cell lines.
|
-
- HY-146159
-
PI3K/HDAC-IN-2
|
PI3K
HDAC
|
Cancer
|
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.
|
-
- HY-10227
-
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-15167A
-
-
- HY-N6820
-
-
- HY-N6819
-
-
- HY-N5146
-
Ophiopogonside A
|
Others
|
Cancer
|
Ophiopogonside A, a natural conpound that could be isolated from ophiopogon japonicas, possesses anti-cancer activity.
|
-
- HY-125825
-
-
- HY-121632
-
Quinoclamine
|
NF-κB
|
Cancer
|
Quinoclamine, a naphthoquinone derivative, is a NF-κB inhibitor. Quinoclamine exhibits anti-cancer activity.
|
-
- HY-16937
-
-
- HY-N10449
-
-
- HY-N9322
-
-
- HY-N0423
-
-
- HY-N4175
-
Cucurbitacin A
|
Others
|
Cancer
|
Cucurbitacin A, a triterpenoid that could be isolated from the Stems of Cucumis melo, shows anti-cancer activity.
|
-
- HY-19909
-
NRC-2694
|
EGFR
|
Cancer
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-N0275
-
-
- HY-N2302
-
-
- HY-N0718
-
-
- HY-104015
-
-
- HY-N1497
-
Plumbagin
2-Methyljuglone
|
Others
|
Cancer
|
Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica L, exhibits anticancer and antiproliferative activities.
|
-
- HY-N9358
-
Argentinogenin
|
Others
|
Cancer
|
Argentinogenin is a natural compound with anti-cancer activity that could be found in traditional Chinese drug Chan Su.
|
-
- HY-N0362
-
-
- HY-N9437
-
-
- HY-N0562
-
-
- HY-130260
-
-
- HY-112710
-
-
- HY-P0173A
-
Chlorotoxin
|
Chloride Channel
|
Cancer
|
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
|
-
- HY-W015084
-
β-Ionone
|
Apoptosis
|
Cancer
|
β-Ionone is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
|
-
- HY-N6814
-
-
- HY-N8190
-
-
- HY-N4326
-
-
- HY-N4252
-
Periplocymarin
|
Others
|
Cancer
|
Periplocymarin, a cardiac glycoside isolated from Periploca sepium and Periploca graeca, is a potential anti-cancer compound.
|
-
- HY-N1423
-
-
- HY-N0038
-
-
- HY-P1592
-
G3-C12
|
Galectin
|
Cancer
|
G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
|
-
- HY-N7667
-
-
- HY-142657
-
PARP1-IN-7
|
PARP
|
Cancer
|
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
|
-
- HY-N1405
-
Cucurbitacin I
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-N8083
-
Icariside B1
|
Others
|
Cancer
|
Icariside B1 is a megastigmane glycoside compound isolated from Petasites tricholobus Franch, with an anticancer effect.
|
-
- HY-N0073
-
-
- HY-149021
-
Tubulin polymerization-IN-28
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research.
|
-
- HY-147271
-
-
- HY-147248
-
Opadotina
|
Others
|
Cancer
|
Opadotina is a small molecule of anvatabart opadotin. Opadotina shows antineoplastic activity.
|
-
- HY-147633
-
-
- HY-147636
-
-
- HY-147303
-
Sacibertinib
|
EGFR
|
Cancer
|
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.
|
-
- HY-142947
-
-
- HY-143266
-
Topoisomerase I inhibitor 3
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
|
-
- HY-N2415
-
Podophyllotoxone
|
Microtubule/Tubulin
|
Cancer
|
Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization.
|
-
- HY-128576
-
DS21360717
|
Others
|
Cancer
|
DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
|
-
- HY-N0472
-
-
- HY-103096
-
R162
|
Others
|
Cancer
|
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
|
-
- HY-135848
-
-
- HY-15097
-
-
- HY-P1592A
-
G3-C12 TFA
|
Galectin
|
Cancer
|
G3-C12 (TFA) is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
|
-
- HY-W012732
-
Isoquinoline
|
Others
|
Cancer
|
Isoquinoline is an analog of pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities.
|
-
- HY-16514
-
Vindesine
|
Others
|
Cancer
|
Vindesine is a semisynthetic derivative of vinblastine. Vindesine is a potent anticancer agent. Vindesine can be used for the research of melanoma and lung cancers.
|
-
- HY-N6658
-
-
- HY-N2343
-
-
- HY-102007
-
Gamitrinib TPP
|
HSP
|
Cancer
|
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-78428
-
CDK-IN-6
|
CDK
|
Cancer
|
CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.
|
-
- HY-146596
-
-
- HY-146657
-
4BAB
|
Others
|
Cancer
|
4BAB (compound 29) is an irreversible glyoxalase I (GLO1) inhibitor. 4BAB has anticancer effects.
|
-
- HY-146241
-
SN40
|
Others
|
Cancer
|
SN40 is a potent amino acid transport (AAT) inhibitor with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 can be used for researching anticancer.
|
-
- HY-N7586
-
-
- HY-P2470
-
-
- HY-N0763
-
Angelicin
Isopsoralen
|
Apoptosis
Virus Protease
|
Cancer
|
Angelicin, a furocoumarin naturally occurring tricyclic aromatic compound, structurally related to psoralens, is reported to have anti-cancer, antiviral, anti-inflammatory activity.
|
-
- HY-N1983
-
Caudatin
|
Apoptosis
|
Cancer
|
Caudatin is a steroidal cmpound found in Cynanchum auriculatum, causes cell cycle arrest and induces apoptosis, with anti-cancer and antiangiogenic properties.
|
-
- HY-N3733
-
Deoxylapachol
|
Fungal
|
Cancer
Infection
|
Deoxylapachol is a major cytotoxic component of New Zealand brown alga, Landsburgia quercifolia. Deoxylapachol has antifungal and anti-cancer activity.
|
-
- HY-W012282
-
-
- HY-144222
-
NSC 828467
|
Others
|
Cancer
|
NSC 828467 exhibited significant in vitro anticancer activity,and it is one of the top-five CA IX inhibitors with an IC50 value of 27.2nM.
|
-
- HY-18668
-
-
- HY-W001023
-
-
- HY-16265
-
-
- HY-145717
-
-
- HY-121323
-
-
- HY-100309
-
9-amino-CPT
9-amino-20(S)-camptothecin
|
Topoisomerase
|
Cancer
|
9-amino-CPT (9-amino-20(S)-camptothecin) is a topoisomerase I inhibitor with potent anticancer activity.
|
-
- HY-N4277
-
Methyl protogracillin
NSC-698793
|
Others
|
Cancer
|
Methyl protogracillin (NSC-698793), isolated from the roots of Dioscorea opposite Thunb, exhibits strong anti-cancer activity.
|
-
- HY-N0500
-
Mogroside III
|
Others
|
Cancer
Metabolic Disease
|
Mogroside III is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-126421
-
-
- HY-100350
-
-
- HY-146636
-
-
- HY-N10367
-
Corydamine
|
Topoisomerase
|
Cancer
|
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity.
|
-
- HY-128447
-
-
- HY-108275
-
Mogroside VI
|
Others
|
Cancer
Metabolic Disease
|
Mogroside VI is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-101790A
-
-
- HY-B1890
-
-
- HY-139058
-
-
- HY-N6855
-
Mogroside IIA1
|
Others
|
Cancer
Metabolic Disease
|
Mogroside IIA1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-137316
-
-
- HY-N2456
-
Mogroside IV-E
|
Others
|
Cancer
Metabolic Disease
|
Mogroside IV-E, a triterpenoid glycoside, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-U00095
-
Hepsulfam
NCI 329680; ZINC01574758
|
Others
|
Cancer
|
Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
|
-
- HY-P0173B
-
Chlorotoxin TFA
|
Chloride Channel
|
Cancer
|
Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker. Anti-cancer activity.
|
-
- HY-102007A
-
Gamitrinib TPP hexafluorophosphate
|
HSP
|
Cancer
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-126288
-
ASTX029
|
ERK
|
Cancer
|
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor. ASTX029 has anti-cancer activity.
|
-
- HY-106541
-
Neticonazole
|
Fungal
|
Cancer
Infection
|
Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole has anti-infection and anti-cancer effects.
|
-
- HY-N0756
-
Bornyl acetate
|
Apoptosis
|
Cancer
|
Bornyl acetate is a potent odorant, exhibiting one of the highest flavor dilution factor (FD factor). Bornyl acetate possesses anti-cancer activity.
|
-
- HY-14603
-
-
- HY-128365
-
-
- HY-B0402A
-
Amantadine hydrochloride
1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
Bcl-2 Family
CDK
|
Cancer
Infection
Neurological Disease
|
Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-B0402
-
Amantadine
1-Adamantanamine; 1-Aminoadamantane
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
CDK
Bcl-2 Family
|
Cancer
Infection
Neurological Disease
|
Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-Y0790
-
Cuminaldehyde
|
Endogenous Metabolite
|
Cancer
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.
|
-
- HY-143430
-
LY3143921
|
CDK
|
Cancer
|
LY3143921 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. LY3143921 shows broad in vitro anticancer activity.
|
-
- HY-121093
-
-
- HY-N0709
-
-
- HY-132607
-
-
- HY-N2698
-
-
- HY-120272
-
SMAP-2
DT-1154
|
Phosphatase
|
Cancer
|
SMAP-2 (DT-1154) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.
|
-
- HY-D0803
-
Thymoquinone
|
Others
|
Inflammation/Immunology
|
Thymoquinone is a nature product isolated from N. sativa. Thymoquinone possess antioxidant, anti-inflammatory, anti-cancer, antitumor activities and hepatoprotective properties.
|
-
- HY-N0105
-
-
- HY-17435
-
4'-Demethylepipodophyllotoxin
4'-O-demethylepipodophyllotoxin; 4'-DMEP
|
Microtubule/Tubulin
|
Cancer
|
4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.
|
-
- HY-126482
-
Telomerase-IN-2
|
Telomerase
|
Cancer
|
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
|
-
- HY-14714
-
-
- HY-17601
-
-
- HY-N2423
-
-
- HY-N6854
-
Mogroside I A1
|
Others
|
Cancer
Metabolic Disease
|
Mogroside I A1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N5089
-
-
- HY-103001
-
HMN-154
|
Others
|
Cancer
|
HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.
|
-
- HY-N6853
-
Mogroside I E1
|
Others
|
Cancer
Metabolic Disease
|
Mogroside I E1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-143430A
-
LY3143921 hydrate
|
CDK
|
Cancer
|
LY3143921 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. LY3143921 hydrate shows broad in vitro anticancer activity.
|
-
- HY-16247
-
Apoptone
HE3235
|
Others
|
Cancer
|
Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer.
|
-
- HY-10227S
-
Bortezomib-d8
PS-341-d8; LDP-341-d8; NSC 681239-d8
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
Bortezomib-d8 (PS-341-d8) is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-146242
-
SN05
|
Others
|
Cancer
|
SN05 is a potent amino acid transport (AAT) inhibitor with Kis of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used for researching anticancer.
|
-
- HY-P1750
-
Shepherdin (79-87)
|
HSP
Survivin
|
Cancer
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
|
-
- HY-N0799
-
Protodioscin
|
Endogenous Metabolite
|
Cancer
|
Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
|
-
- HY-W011303
-
-
- HY-124669
-
RTC-30
|
Others
|
Cancer
|
RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability.
|
-
- HY-N10457
-
Norstictic acid
|
Bacterial
|
Cancer
Infection
|
Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity.
|
-
- HY-108272
-
Mogroside II-A2
|
Others
|
Cancer
Metabolic Disease
|
Mogroside II-A2 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-W013573
-
-
- HY-43058
-
5'-O-DMT-ibu-rG
5'-O-DMT-N2-isobutyrylguanosine
|
Others
|
Others
|
5'-O-DMT-ibu-rG is a useful model for a new class of DNA binding molecules for the development of potent and selective anti-cancer agents.
|
-
- HY-N3500
-
-
- HY-123786
-
NSC745887
|
Others
|
Cancer
|
NSC745887 (compound 25) is an anti-cancer agent. NSC745887 exhibits dose-dependent inhibition of proliferation in all 60 cancer cell lines.
|
-
- HY-N0330
-
Momordin Ic
|
Apoptosis
|
Cancer
|
Momordin Ic is a principal saponin constituent of Fructus Kochiae, with with anti-cancer bioactivity. Momordin Ic induces apoptosis through oxidative stress-regulated mitochondrial dysfunction.
|
-
- HY-137316A
-
-
- HY-N6821
-
-
- HY-14615
-
[6]-Gingerol
(S)-(+)-[6]Gingerol; 6-Gingerol
|
AMPK
Apoptosis
|
Cancer
|
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
|
-
- HY-13748
-
Silibinin
Silibinin A; Silymarin I
|
Autophagy
Reactive Oxygen Species
|
Cancer
|
Silibinin (Silibinin A), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
|
-
- HY-111621
-
DC661
|
Autophagy
Apoptosis
|
Cancer
|
DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
|
-
- HY-N0697
-
-
- HY-N6998
-
Paederosidic acid
|
Apoptosis
|
Cancer
|
Paederosidic acid is isolated from P. scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis.
|
-
- HY-B0299
-
Oxibendazole
|
Parasite
Apoptosis
|
Infection
|
Oxibendazole is an effective benzimidazole anthelmintic and is against nema-tode infections. Oxibendazole can induces apoptosis and has anti-cancer and anti-inflammation activities.
|
-
- HY-108271
-
Mogroside III-A1
|
Others
|
Cancer
Metabolic Disease
|
Mogroside III-A1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N2039
-
-
- HY-B0402B
-
Amantadine sulfate
1-Adamantanamine sulfate; 1-Aminoadamantane sulfate
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
CDK
Bcl-2 Family
|
Cancer
Infection
Neurological Disease
|
Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-121222
-
alpha-Bisabolol
|
Apoptosis
|
Cancer
|
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
|
-
- HY-N6781
-
Ophiobolin A
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-111758
-
PROTAC B-Raf degrader 1
|
PROTACs
Raf
|
Cancer
|
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
|
-
- HY-N2994
-
-
- HY-N6877
-
Purpurogallin carboxylic acid
|
Others
|
Cancer
|
Purpurogallin carboxylic acid, isolated from Macleaya microcarpa (Maxim.) Fedde, is an oxidation product of gallic acid in fermented tea. Purpurogallin carboxylic acid has anti-cancer activity.
|
-
- HY-117152
-
L-threo-Sphingosine
L-threo-Sphingosine C-18
|
p38 MAPK
Apoptosis
|
Cancer
|
L-threo-Sphingosine is a potent MAPK inhibitor. L-threo-Sphingosine induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine shows anticancer effect.
|
-
- HY-N0248
-
Saikosaponin B2
|
HCV
|
Cancer
Infection
|
Saikosaponin B2 is an active component from Bupleurum kaoi root, acts as an entry inhibitor against HCV infection. Anti-cancer activity.
|
-
- HY-B0134
-
-
- HY-N6637
-
Senecionine N-oxide
|
Others
|
Cancer
|
Senecionine n-oxide is the primary product of pyrrolizidine alkaloid biosynthesis in root cultures of Senecio vulgaris. Senecionine N-oxide has anti-cancer activity.
|
-
- HY-108932
-
Gemcitabine monophosphate
Gemcitabine 5′-phosphate
|
Apoptosis
|
Cancer
|
Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate shows synergistic anti-cancer effects.
|
-
- HY-14616
-
Shogaol
[6]-Shogaol; 6-Shogaol
|
Autophagy
|
Cancer
|
Shogaol ([6]-Shogaol), an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
|
-
- HY-116514
-
-
- HY-N5014
-
-
- HY-B0018
-
Docetaxal
10-Acetyl docetaxel; PNU-101383
|
Others
|
Cancer
|
Docetaxal (10-Acetyl docetaxel) is an analog of Docetaxel (HY-B0011), with anticancer activity. Docetaxel is a microtubule disassembly inhibitor, with antimitotic activity.
|
-
- HY-107470
-
-
- HY-118474
-
GW 610
NSC 721648
|
Others
|
Cancer
|
GW 610 (NSC 721648), an antitumor agent, shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines.
|
-
- HY-N2032
-
Euphorbiasteroid
|
AMPK
|
Cancer
Infection
Metabolic Disease
|
Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
|
-
- HY-15995
-
-
- HY-N0124
-
Dioscin
Collettiside III; CCRIS 4123
|
Autophagy
Apoptosis
|
Cancer
|
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines.
|
-
- HY-136217
-
PU 23
|
Others
|
Cancer
|
PU 23 is a non-carboxylic multidrug resistance protein 4 (MRP4) inhibitor as an active agent reducing resistance to anticancer agent 6-Mercaptopurine.
|
-
- HY-N0252
-
-
- HY-N0401
-
-
- HY-150615
-
SphK1-IN-2
|
SphK
Apoptosis
|
Cancer
|
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and >10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.
|
-
- HY-143442
-
-
- HY-146587
-
Haspin-IN-2
|
Haspin Kinase
CDK
DYRK
|
Cancer
|
Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC50 of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 445 nM and 917 nM, respectively.
|
-
- HY-146492
-
VEGFR-2/BRAF-IN-2
|
VEGFR
Raf
Apoptosis
|
Cancer
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase.
|
-
- HY-126373
-
SN-38 glucuronide
SN-38G
|
Others
|
Cancer
|
SN-38 glucuronide is an inactive metabolite of the cancer drug Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer.
|
-
- HY-143440
-
-
- HY-146491
-
VEGFR-2/BRAF-IN-1
|
VEGFR
Raf
Apoptosis
|
Cancer
|
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase.
|
-
- HY-146178
-
IMP2-IN-1
|
Others
|
Cancer
|
IMP2-IN-1 (compound 4) is a potent IMP2 inhibitor with IC50 value of 81.3~127.5 for IMP2 RNA sequence. IMP2-IN-1 reduces IMP2 in SW480 cells. IMP2-IN-1 significantly reduces the viability of both differentiated and non-differentiated Huh7 cells.
|
-
- HY-137457
-
Venadaparib
IDX-1197
|
PARP
|
Cancer
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research.
|
-
- HY-143441
-
-
- HY-146501
-
PARP10/15-IN-2
|
PARP
Apoptosis
|
Cancer
|
PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis.
|
-
- HY-150731
-
-
- HY-146502
-
PARP10/15-IN-3
|
PARP
Apoptosis
|
Cancer
|
PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.14 µM and 0.40 µM against PARP10 and PARP15, respectively. PARP10/15-IN-3 is able to enter cells and rescue cells from apoptosis.
|
-
- HY-146252
-
-
- HY-124833
-
Quinalizarin
|
Casein Kinase
|
Cancer
|
Quinalizarin is a potent, selective and cell-permeable protein kinase CK2 inhibitor with an Ki of ~50 nM and an IC50 of 110 nM. Quinalizarin can induce apoptosis of certain cancer cells.
|
-
- HY-145703
-
-
- HY-146586
-
Haspin-IN-1
|
Haspin Kinase
CDK
DYRK
|
Cancer
|
Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC50 of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 221 nM and 916.3 nM, respectively.
|
-
- HY-138946
-
XY028-140
|
CDK
PROTACs
|
Cancer
|
XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.
|
-
- HY-120940
-
AZ13705339
|
PAK
|
Cancer
|
AZ13705339 is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 has moderate clearance in rat hepatocytes (CLint = 30 µL/min/10^6).
|
-
- HY-N0779A
-
Silybin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Silybin is a flavonolignan isolated from milk thistle (Silybum marianum) seeds. Silybin induces apoptosis and exhibits hepatoprotective, antioxidant, anti-inflammatory, anti-cancer activity.
|
-
- HY-B0790
-
TAI-1
|
Apoptosis
|
Cancer
|
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
|
-
- HY-122965
-
Batatasin III
|
FAK
Akt
|
Cancer
|
Batatasin III, a stilbenoid, inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition (EMT) and FAK-AKT signals. Batatasin III has anti-cancer activities.
|
-
- HY-13777
-
Zoledronic Acid
Zoledronate; CGP 42446; CGP42446A; ZOL 446
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
|
-
- HY-N6621
-
Hippeastrine
|
Topoisomerase
|
Cancer
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities.
|
-
- HY-N8405
-
Isolimonexic acid
|
Aromatase
|
Cancer
|
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
|
-
- HY-13777A
-
Zoledronic acid monohydrate
Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
|
-
- HY-N0252A
-
-
- HY-N7494
-
Pentacosane
|
Others
|
Cancer
|
Pentacosane is one of the major components in the acetone extract from Curcuma raktakanda and is also in the essential oil from the leaves of Malus domestica. Pentacosane exhibit anti-cancer activities.
|
-
- HY-16942
-
Damulin B
|
Apoptosis
|
Cancer
|
Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum.Damulin B can induce cell apoptosis and has anti-cancer activities in vitro.
|
-
- HY-N2193
-
Hirsutine
|
Apoptosis
|
Cancer
Infection
|
Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.
|
-
- HY-107632
-
-
- HY-N8398
-
n-Octyl caffeate
|
Apoptosis
|
Cancer
|
n-Octyl caffeate shows anti-cancer and apoptosis inducing activity in highly liver-metastatic murine colon 26-L5 carcinoma cell lines.
|
-
- HY-N2058
-
Neogambogic acid
|
Bacterial
Apoptosis
|
Cancer
Infection
|
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA).
|
-
- HY-111343
-
ONC212
|
Apoptosis
|
Cancer
Endocrinology
|
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
|
-
- HY-136552
-
β-Bisabolene
|
Others
|
Cancer
|
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer.
|
-
- HY-101191
-
Ecteinascidin 770
Ecteinascidine 770; Et-770
|
Apoptosis
|
Cancer
|
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
|
-
- HY-17393
-
-
- HY-115604
-
Pitstop 2
|
Apoptosis
|
Cancer
|
Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research.
|
-
- HY-136203
-
-
- HY-N1443
-
-
- HY-N0007S
-
Bisdemethoxycurcumin-d8
Curcumin III-d8; Didemethoxycurcumin-d8
|
Apoptosis
Autophagy
|
Cancer
|
Bisdemethoxycurcumin-d8 (Curcumin III-d8) is the deuterium labeled Bisdemethoxycurcumin. Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
|
-
- HY-P2228
-
Chlamydocin
|
HDAC
Apoptosis
|
Cancer
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
|
-
- HY-N1423S1
-
Glycocholic acid-d5
|
Endogenous Metabolite
|
Cancer
|
Glycocholic acid-d5 is the deuterium labeled Glycocholic acid. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
|
-
- HY-N6945
-
Mogroside IV
|
Others
|
Cancer
Metabolic Disease
|
Mogroside IV, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-111838A
-
ZZW-115 hydrochloride
|
Apoptosis
|
Cancer
|
ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-111838
-
ZZW-115
|
Apoptosis
|
Cancer
|
ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-100618
-
-
- HY-136204
-
-
- HY-132254
-
-
- HY-12484
-
BMH-21
|
DNA/RNA Synthesis
|
Cancer
|
BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity.
|
-
- HY-10448
-
-
- HY-N1375
-
Qingyangshengenin
|
Others
|
Cancer
|
Qingyanshengenin (NSC 379666; compound 2), a pregnane glycoside, is a C21 steroidal aglycone isolated from the root of Cynanchumot ophyllum (Asclepiadaceae). Qingyanshengenin has anti-cancer activity.
|
-
- HY-125727
-
Globosuxanthone A
|
Fungal
|
Cancer
Infection
|
Globosuxanthone A is a dihydroxanthenone with obvious antifungal activity towards Fusarium graminearum, Fusarium solani, and Botrytis cinerea with MIC values of 4, 8, and 16 μg/mL, respectively. Anticancer activity.
|
-
- HY-N6942
-
Mogroside IV-A
|
Others
|
Cancer
Metabolic Disease
|
Mogroside IV-A, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-146026
-
-
- HY-18974
-
-
- HY-19118
-
KP1019
FFC14A
|
Apoptosis
|
Cancer
|
KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer agent. KP1019 induces DNA damage and apoptosis in cancer cells.
|
-
- HY-14804A
-
Tasisulam sodium
LY 573636 sodium
|
Apoptosis
|
Cancer
|
Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
|
-
- HY-139011
-
IV-361
|
CDK
|
Cancer
|
IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).
|
-
- HY-136447
-
ASP4132
|
AMPK
|
Cancer
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
|
-
- HY-135957
-
-
- HY-13735B
-
Quinacrine hydrochloride hydrate
Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Cancer
Infection
|
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
|
-
- HY-N4127
-
3'-Demethylnobiletin
|
Others
|
Cancer
|
3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits. Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling.
|
-
- HY-125974
-
HM03
|
HSP
|
Cancer
|
HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
|
-
- HY-N0453S
-
Hypericin-d10
|
Apoptosis
Influenza Virus
|
Cancer
|
Hypericin-d10 is the deuterium labeled Hypericin. Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM.
|
-
- HY-N7678
-
Gypenoside LXXV
|
Others
|
Cancer
|
Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect.
|
-
- HY-125974A
-
HM03 trihydrochloride
|
HSP
|
Cancer
|
HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity.
|
-
- HY-101085
-
SKL2001
|
Wnt
β-catenin
|
Cancer
|
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
|
-
- HY-N2065
-
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-143320
-
STING agonist-17
|
STING
|
Cancer
|
STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
|
-
- HY-N0332
-
-
- HY-125006
-
TRi-1
|
Others
|
Cancer
|
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
|
-
- HY-14804
-
Tasisulam
LY 573636
|
Apoptosis
|
Cancer
|
Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
|
-
- HY-143424
-
MALT1-IN-6
|
MALT1
|
Cancer
|
MALT1-IN-6 is a potent MALT1 protease inhibitor with a Ki of 9 nM. MALT1-IN-6 has anticancer effects (WO2018226150A1; Compound 4).
|
-
- HY-14618
-
Zingiberene
α-Zingiberene; (-)-Zingiberene
|
Autophagy
|
Cancer
|
Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential. Zingiberene triggers autophagy. Anticancer activity.
|
-
- HY-N4114
-
Picrocrocin
|
Apoptosis
|
Cancer
|
Picrocrocin, an apocarotenoid found in the flowers of Cochliobolus sativus. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells.
|
-
- HY-19530
-
PF-2771
|
Kinesin
|
Cancer
|
PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC50 of 16.1 nM; PF-2771 is used as an anticancer agent.
|
-
- HY-147059
-
-
- HY-136711
-
-
- HY-U00141
-
ABTL-0812
α-Hydroxylinoleic acid
|
Autophagy
|
Metabolic Disease
|
ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
|
-
- HY-N0737
-
-
- HY-147888
-
Tubulin inhibitor 29
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site.
|
-
- HY-N0565
-
Doxycycline
|
MMP
Bacterial
Antibiotic
|
Cancer
Infection
|
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor. Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity.
|
-
- HY-N8431
-
-
- HY-113462
-
α-Carotene
|
Others
|
Cancer
|
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. α-Carotene is isolated from yellow-orange and dark-green vegetables.
|
-
- HY-N0565A
-
-
- HY-N2599
-
Taraxerol acetate
|
COX
Apoptosis
|
Cancer
|
Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.
|
-
- HY-N10392
-
(S)-Erypoegin K
|
Apoptosis
|
Cancer
|
(S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis.
|
-
- HY-136901
-
-
- HY-N0502
-
Mogroside V
|
Others
|
Cancer
Metabolic Disease
|
Mogroside V is a triterpenoid glycoside and a nonsugar sweetener. Mogroside V is nearly 300 times sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities. Mogrosides are sweeter than sucrose.
|
-
- HY-141478
-
Antitumor agent-28
|
ATM/ATR
|
Cancer
|
Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.
|
-
- HY-15287
-
Nelfinavir
AG1341
|
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
|
-
- HY-146164
-
-
- HY-139017
-
-
- HY-N2303
-
-
- HY-111617
-
BTR-1
|
Apoptosis
|
Cancer
|
BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
|
-
- HY-131503
-
13-Methyltetradecanoic acid
13-MTD; 13-Methylmyristic acid
|
Apoptosis
|
Cancer
|
13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells.
|
-
- HY-W047478
-
3-Methylcarbazole
NSC 10154
|
Others
|
Cancer
|
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitory activity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells.
|
-
- HY-15287A
-
Nelfinavir Mesylate
AG 1343 Mesylate
|
HIV Protease
HIV
|
Cancer
Infection
|
Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
|
-
- HY-100888
-
Simurosertib
TAK-931
|
CDK
|
Cancer
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
|
-
- HY-13735A
-
Quinacrine dihydrochloride
Mepacrine dihydrochloride; SN-390 dihydrochloride
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Cancer
Infection
|
Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
|
-
- HY-126490
-
Phleomycin
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Cancer
Infection
|
Phleomycin is an anticancer glycopeptide antibiotic found in Streptomyces verticillus, which cause DNA cleavage. Phleomycin binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A).
|
-
- HY-121027
-
Anagyrine
(-)-Anagyrine; Monolupine; Rhombinine
|
mAChR
nAChR
|
Cancer
|
Anagyrine is an alkaloid that has been found in L. albus and has nematocidal and anticancer activities.It binds to muscarinic and nicotinic acetylcholine receptors (AChRs) with IC50 values of 132 and 2096 µM respectively.
|
-
- HY-P1539A
-
-
- HY-N2460
-
Aloesin
Aloeresin
|
Others
|
Cancer
Inflammation/Immunology
|
Aloesin (Aloeresin) is an active constituent of the herb aloe vera and displays anti-inflammatory activity, ultraviolet protection, and antibacterium effects. Aloesin exerts its anticancer effect through the MAPK signaling pathway.
|
-
- HY-129558
-
UK-1
|
HCV
|
Cancer
Infection
|
UK-1 is a cytotoxic metabolite from Streptomyces sp. 517-02 and exerts a wide spectrum of potent anticancer activities. UK-1 also inhibits HCV replication.
|
-
- HY-U00442
-
CTX1
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
|
-
- HY-N7512
-
Asimilobine
|
Dopamine Receptor
5-HT Receptor
Parasite
|
Cancer
Infection
|
Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
|
-
- HY-121368
-
Mahanine
|
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
Mahanine is a carbazole alkaloid with various biological properties. Mahanine is a potent anticancer agent against different types of cancer cells. Mahanine exhibits antileishmanial activity and can be used for Leishmania infection treatment research.
|
-
- HY-N0709S
-
Coumarin-d4
|
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
Coumarin-d4 is the deuterium labeled Coumarin. Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
|
-
- HY-N0808
-
-
- HY-130978
-
Duocarmycin DM
|
DNA Alkylator/Crosslinker
ADC Cytotoxin
|
Cancer
|
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.
|
-
- HY-147572
-
BET-IN-10
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-10 is a BET inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC50 of 26.5 nM (WO2022012456A1; example 6).
|
-
- HY-145513
-
CL2-MMT-SN38
|
Topoisomerase
|
Cancer
|
CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11).
|
-
- HY-139017A
-
-
- HY-122903A
-
(-)-TK216
|
DNA/RNA Synthesis
|
Cancer
|
(-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity.
|
-
- HY-N2575
-
Hypocrellin A
|
PKC
Bacterial
Parasite
|
Cancer
Infection
|
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).
|
-
- HY-147776
-
Antiproliferative agent-8
|
MDM-2/p53
|
Cancer
|
Antiproliferative agent-8 (Compound 5a) is an anti-cancer agent. Antiproliferative against-8 has antiproliferative activity. Antiproliferative agent-8 significantly increases the P53 levels.
|
-
- HY-150794
-
FLDP-8
|
Others
|
Cancer
|
FLDP-8 is a curcuminoid analogues, has potent anti-cancer effects. FLDP-8 can induce cell death with an IC50 value of 4 μM in LN-18 cells.
|
-
- HY-N0820
-
-
- HY-N0565B
-
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Cancer
Infection
|
Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor. Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity.
|
-
- HY-N4149
-
Quercetagetin
6-Hydroxyquercetin
|
Pim
|
Cancer
Inflammation/Immunology
|
Quercetagetin (6-Hydroxyquercetin) is a flavonoid. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.
|
-
- HY-N0929
-
Hexahydrocurcumin
|
COX
Reactive Oxygen Species
|
Cancer
|
Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities.
|
-
- HY-139453
-
LP-184
|
Others
|
Cancer
|
LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
|
-
- HY-114429
-
CB-6644
|
Others
|
Cancer
|
CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.
|
-
- HY-N2477
-
Taraxerol
|
Apoptosis
NF-κB
|
Cancer
Inflammation/Immunology
|
Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.
|
-
- HY-N6012
-
(-)-Alkannin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
(-)-Alkannin, found in Alkanna tinctoria, is used as a food coloring. (-)-Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. (-)-Alkannin improves hepatic inflammation in a Rho-kinase pathway.
|
-
- HY-147185
-
-
- HY-107805
-
Dihydroactinidiolide
|
Others
|
Cancer
Infection
Neurological Disease
|
Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect.
|
-
- HY-N0770
-
Isoliensinine
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells.
|
-
- HY-N0565C
-
-
- HY-N2113
-
Glaucocalyxin B
|
Autophagy
|
Cancer
|
Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 h.
|
-
- HY-N0064
-
-
- HY-125759
-
3-Phenyltoxoflavin
|
HSP
|
Cancer
|
3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity.
|
-
- HY-N0616
-
Trifolirhizin
|
Tyrosinase
|
Cancer
Inflammation/Immunology
|
Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitory activity with an IC50 of 506 μM. Trifolirhizin exhibits potential anti-inflammatory and anticancer activities.
|
-
- HY-N4084
-
Thonningianin A
|
Apoptosis
|
Cancer
|
Thonningianin A, an ellagitannin, is isolated from the methanolic extract of the African medicinal herb, Thonningia sanguinea. The antioxidant properties of Th A involve radical scavenging, anti-superoxide formation and metal chelation. Anti-cancer activities.
|
-
- HY-P9958
-
Denosumab
Immunoglobulin G2; Ranmark
|
NF-κB
|
Cancer
|
Denosumab is a human monoclonal antibody binding to, and inhibiting, the receptor activator of RANKL (TNFSF11). Denosumab can reduce the risk of vertebral, nonvertebral and hip fractures, also has anti-cancer activity.
|
-
- HY-N0252B
-
Catharanthine Sulfate
(+)-3,4-Didehydrocoronaridine Sulfate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
Catharanthine Sulfate ((+)-3,4-Didehydrocoronaridine Sulfate) is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activities.
|
-
- HY-101796
-
NSC-70220
|
Others
|
Cancer
|
NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
|
-
- HY-129459
-
-
- HY-119874
-
Alkannin
|
Ras
|
Cancer
Inflammation/Immunology
|
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
|
-
- HY-N0290
-
Mangiferin
|
NF-κB
Keap1-Nrf2
Apoptosis
|
Cancer
|
Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities.
|
-
- HY-136977
-
EEDi-5285
|
Histone Methyltransferase
|
Cancer
|
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
|
-
- HY-B1115A
-
-
- HY-N1963
-
Curzerene
|
Gutathione S-transferase
Apoptosis
|
Cancer
|
Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
|
-
- HY-13250
-
Silvestrol aglycone
|
Others
|
Cancer
|
Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
|
-
- HY-N1925
-
Tea polyphenol
|
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
Tea polyphenol is the floorboard of phenolic compounds in tea. Tea polyphenol exhibits biological activity including antioxidant and anti-cancer activities, inhibition of cell proliferation, induction of apoptosis, cell cycle arrest and modulation of carcinogen metabolism.
|
-
- HY-103159
-
1-Deazaadenosine
|
Adenosine Deaminase
|
Cancer
|
1-Deazaadenosine is a potent Adenosine deaminase (ADA) inhibitor with a Ki value of 0.66 μM. 1-Deazaadenosine exhibits anti-cancer activities in vitro and has the potential to be a chemotherapy agent for lymphoproliferative disorders.
|
-
- HY-128669
-
-
- HY-16172
-
DMAPT
Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
|
-
- HY-109115
-
Fosifloxuridine nafalbenamide
NUC-3373
|
Thymidylate Synthase
|
Cancer
|
Fosifloxuridine nafalbenamide (NUC-3373), a pyrimidine nucleotide analogue, is a Thymidylate synthase inhibitor. Fosifloxuridine nafalbenamide has anticancer activity. Fosifloxuridine nafalbenamide has the potential to evoke a host immune response and enhance immunotherapy.
|
-
- HY-113825
-
CLK1/2-IN-1
|
CDK
|
Cancer
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 16 nM and 45 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities[1] .
|
-
- HY-100556
-
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-126322
-
DVD-445
|
Others
|
Cancer
|
DVD-445 (Compound 7) is a potent peptidomimetic covalent thioredoxin reductase 1 (TrxR1) inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application.
|
-
- HY-13777B
-
Zoledronic acid disodium tetrahydrate
Zoledronate disodium tetrahydrate; CGP 42446 disodium tetrahydrate; CGP42446A disodium tetrahydrate; ZOL 446 disodium tetrahydrate
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects.
|
-
- HY-N0800
-
Protosappanin B
(-)-Protosappanin B
|
Apoptosis
|
Cancer
|
Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells.
|
-
- HY-13629
-
-
- HY-13768C
-
Topotecan hydrochloride hydrate
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
|
-
- HY-135236
-
OXFBD04
|
Epigenetic Reader Domain
|
Cancer
|
OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.
|
-
- HY-N6866
-
-
- HY-N4187
-
-
- HY-124855
-
-
- HY-147898
-
PI3K-IN-33
|
PI3K
Apoptosis
|
Cancer
|
PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research.
|
-
- HY-142948
-
-
- HY-147899
-
PI3K-IN-34
|
PI3K
Apoptosis
|
Cancer
|
PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research.
|
-
- HY-146037
-
-
- HY-143431
-
Cdc7-IN-17
|
CDK
|
Cancer
|
Cdc7-IN-17 is a potent CDC7 inhibitor with an IC50 of <10 μM, extracted from patent WO2018217439A1. Cdc7-IN-17 can be used for cancer research.
|
-
- HY-115994
-
Carbonic anhydrase inhibitor 10
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research.
|
-
- HY-146387
-
SIRT5 inhibitor 3
|
Sirtuin
|
Cancer
Neurological Disease
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-147580
-
BTK-IN-10
|
Btk
|
Cancer
|
BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111).
|
-
- HY-147917
-
RNA polymerase II-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
RNA polymerase II-IN-2 (compound 20iii) is a potent RNA polymerase II (Pol II) inhibitor with Ki value of 9.5 nM. RNA polymerase II-IN-2 has cytotoxicity against cancer cells, and exhibits 2 and 5 fold toxicity than α-amanitin against CHO and HEK293.
|
-
- HY-124663
-
-
- HY-145330
-
NSC639828
|
DNA/RNA Synthesis
|
Cancer
|
NSC639828 is a potent inhibitor of DNA polymerase α with an IC50 of 70 μM. NSC639828 has high antitumor activity. NSC639828 has the potential for researching cancer disease.
|
-
- HY-147021A
-
-
- HY-124573
-
OBI-3424
TH-3424
|
DNA Alkylator/Crosslinker
|
Cancer
|
OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
|
-
- HY-118946B
-
BPH-1358 mesylate
NSC50460 mesylate
|
Bacterial
|
Cancer
Infection
|
BPH-1358 mesylate (NSC50460 mesylate) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively. BPH-1358 mesylate is active against S. aureus in vitro (MIC ~250 ng/mL).
|
-
- HY-147900
-
PI3K-IN-35
|
PI3K
Apoptosis
|
Cancer
|
PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research.
|
-
- HY-147867
-
MMP-2/9-IN-1
|
MMP
|
Cancer
|
MMP-2/9-IN-1 (Compound 4a) is a potent dual MMP-2 and MMP-9 inhibitor with IC50 values of 56 nM and 38 nM, respectively. MMP-2/9-IN-1 inhibits tumor growth, strongly induces cancer cell apoptosis, inhibits cell migration, and suppresses cell cycle progression leading to DNA fragmentation.
|
-
- HY-N2117
-
-
- HY-146386
-
SIRT5 inhibitor 2
|
Sirtuin
|
Cancer
Neurological Disease
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-149017
-
Apoptosis inducer 7
|
Apoptosis
|
Cancer
|
Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity.
|
-
- HY-12866B
-
-
- HY-147021
-
-
- HY-146474
-
EGFR-IN-54
|
EGFR
|
Cancer
|
EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines.
|
-
- HY-147582
-
BTK-IN-12
|
Btk
|
Cancer
|
BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8).
|
-
- HY-146473
-
EGFR-IN-53
|
EGFR
|
Cancer
|
EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor with an IC50 of 8.264 µM. EGFR-IN-53 shows cytotoxic activity against cancer cell lines.
|
-
- HY-16106A
-
(8R,9S)-Talazoparib
(8R,9S)-BMN-673; (8R,9S)-LT-673
|
PARP
|
Cancer
|
(8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib. (8R,9S)-Talazoparib is an PARP1 inhibitor, with an IC50 of 144 nM.
|
-
- HY-149007
-
STAT3-IN-11
|
STAT
Apoptosis
|
Cancer
|
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers.
|
-
- HY-W016586
-
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N0691
-
Schisandrin
Schizandrin; Schizandrol; Schizandrol-A
|
Autophagy
|
Inflammation/Immunology
Cancer
|
Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats.
|
-
- HY-N5024
-
Gambogenic acid
|
Histone Methyltransferase
|
Cancer
|
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination.
|
-
- HY-136526
-
BCR-ABL-IN-3
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity.
|
-
- HY-N6845
-
3-Isomangostin
|
DNA/RNA Synthesis
|
Cancer
|
3-Isomangostin, extracted from Garciniamangostana.L. shell, is a potent MutT homologue 1 (MTH1) inhibitor with an IC50 value of 52 nM. 3-Isomangostin would be an attractive chemical tool for the development of anticancer agents.
|
-
- HY-116213
-
-
- HY-N2059
-
Santalol
|
Others
|
Cancer
|
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
|
-
- HY-122778
-
δ-Tocotrienol
|
Others
|
Cancer
Neurological Disease
Cardiovascular Disease
|
δ-Tocotrienol is a Vitamin E in vegetables, fruits, seeds, nuts, grains and oils. Vitamin E has become well known for its role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
|
-
- HY-16662
-
Oncrasin-1
|
Ras
Apoptosis
|
Cancer
|
Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells.
|
-
- HY-106423
-
Mivobulin
NSC 613862; (S)-(-)-NSC 613862
|
Microtubule/Tubulin
|
Cancer
|
Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity.
|
-
- HY-W016586A
-
Acivicin hydrochloride
AT-125 hydrochloride; U-42126 hydrochloride
|
Parasite
|
Cancer
Infection
|
Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N2010
-
-
- HY-108695
-
Enterodiol
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Anti-cancer activities.
|
-
- HY-133511
-
MLS000544460
|
Phosphatase
|
Cancer
|
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
|
-
- HY-125166
-
DB04760
|
MMP
|
Cancer
Neurological Disease
|
DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity.
|
-
- HY-147699
-
FRα-IN-1
|
Antifolate
|
Cancer
|
FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
|
-
- HY-16373
-
CP-609754
LNK-754; OSI-754
|
Farnesyl Transferase
|
Cancer
|
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL.
|
-
- HY-N0364
-
-
- HY-N1417
-
Sesamol
|
Apoptosis
|
Cancer
|
Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities. Anticancer activities.
|
-
- HY-121309
-
Doxorubicinone
Adriamycin aglycone; Adriamycinone
|
Endogenous Metabolite
|
Cancer
|
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
|
-
- HY-100003
-
ML-210
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
ML-210 is a selective and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity.
|
-
- HY-117235
-
-
- HY-100865
-
BPR1K871
DBPR114
|
FLT3
|
Cancer
|
BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy.
|
-
- HY-150401
-
Exatecan-amide-cyclopropanol
|
Others
|
Cancer
|
Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively.
|
-
- HY-N0003
-
Honokiol
NSC 293100
|
Akt
Autophagy
HCV
ERK
|
Cancer
|
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
|
-
- HY-113670
-
CLK1/2-IN-2
|
CDK
|
Cancer
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 1.1 nM and 2.4 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities[1] .
|
-
- HY-B0114
-
-
- HY-128915
-
-
- HY-109174
-
Fosciclopirox
CPX-POM
|
γ-secretase
|
Cancer
Metabolic Disease
|
Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
|
-
- HY-N2590
-
Lupenone
|
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
Lupenone, isolated from Rhizoma Musae, belongs to lupane type triterpenoids. Lupenone shows various pharmacological activities including anti-inflammatory, anti-virus, anti-diabetes, anti-cancer, improving Chagas disease without major toxicity.
|
-
- HY-132202
-
-
- HY-123604A
-
TH1834 dihydrochloride
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
|
-
- HY-108639
-
MIRA-1
NSC 19630
|
MDM-2/p53
Apoptosis
|
Cancer
|
MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity.
|
-
- HY-10079
-
CHS-828
GMX1778
|
NAMPT
Apoptosis
|
Cancer
|
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity.
|
-
- HY-103018
-
Gusacitinib
ASN-002
|
JAK
Syk
|
Cancer
|
Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
|
-
- HY-128577
-
NIC3
|
Others
|
Cancer
|
NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity.
|
-
- HY-108969
-
Pyrazoloacridine
NSC 366140; PD 115934
|
Topoisomerase
Apoptosis
|
Cancer
|
Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
|
-
- HY-115737
-
L-threo-PPMP
|
Apoptosis
|
Cancer
|
L-threo-PPMP is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP has anti-cancer activity.
|
-
- HY-N0698
-
-
- HY-130607
-
-
- HY-10454
-
Delanzomib
CEP-18770
|
Proteasome
NF-κB
Apoptosis
|
Cancer
|
Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.
|
-
- HY-N3376
-
Liriodenine
Spermatheridine; VLT045
|
Apoptosis
|
Cancer
|
Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
|
-
- HY-123604
-
TH1834
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
|
-
- HY-143427
-
MALT1-IN-9
|
MALT1
|
Cancer
|
MALT1-IN-9 is a potent MALT1 protease inhibitor with a IC50 of <500 nM in Raji MALT1-GloSensor cells. MALT1-IN-9 has anticancer effects (WO2021000855A1; Compound 5).
|
-
- HY-B0077S
-
Bendamustine-d4 hydrochloride
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Bendamustine-d4 hydrochloride is the deuterium labeled Bendamustine hydrochloride. Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-B0077S1
-
Bendamustine-d8 hydrochloride
SDX-105-d8
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-141701
-
mTOR/HDAC-IN-1
|
mTOR
HDAC
|
Cancer
|
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent.
|
-
- HY-N10358
-
3-(2-Hydroxyethyl) thio withaferin A
|
NF-κB
|
Others
|
3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-136285
-
CPI-1612
|
Histone Acetyltransferase
|
Cancer
|
CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity.
|
-
- HY-N6714
-
Alternariol
|
Topoisomerase
|
Cancer
Infection
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
|
-
- HY-N2521
-
Tetramethylcurcumin
FLLL31
|
STAT
Apoptosis
|
Cancer
Inflammation/Immunology
|
Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects.
|
-
- HY-N7015
-
Zerumbone
|
HSV
|
Infection
|
Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
|
-
- HY-118581
-
Coralyne chloride
|
Topoisomerase
|
Cancer
|
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.
|
-
- HY-N0013
-
-
- HY-12406
-
VLX600
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity.
|
-
- HY-B0134S
-
-
- HY-113805
-
MC70
|
P-glycoprotein
|
Cancer
|
MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC50 of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1.
|
-
- HY-18370
-
-
- HY-19316
-
NU2058
O6-(Cyclohexylmethyl)guanine
|
CDK
|
Cancer
|
NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
|
-
- HY-13768
-
Topotecan
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
|
Cancer
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
|
-
- HY-123464
-
RBC10
|
Ras
|
Cancer
|
RBC10 is an anti-cancer agent. RBC10 inhibits the binding of Ral to its effector RALBP1. RBC10 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines.
|
-
- HY-N7496
-
Odoroside A
|
Apoptosis
|
Cancer
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-N2116
-
Ginkgolic acid C17:1
|
PTEN
Phosphatase
|
Cancer
|
Ginkgolic acid C17:1, extracted from Ginkgo biloba Leaves, suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid C17:1 has anticancer effects.
|
-
- HY-123242
-
FTI-2153
|
Farnesyl Transferase
|
Cancer
|
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
|
-
- HY-N6980
-
Licorice glycoside C2
|
Others
|
Cancer
Infection
|
Licorice glycoside C2 is a oleanane-type triterpene oligoglycoside isolated from Glycyrrhiza uralensis. Various biological activities are associated with licorice extracts, such as anti-viral, anti-microbial, antioxidant, anti-inflammatory, anti-ulcer, anti-cancer and anti-HIV effects.
|
-
- HY-N0720
-
Neobavaisoflavone
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.
|
-
- HY-N5091
-
-
- HY-P0027
-
Jasplakinolide
|
Arp2/3 Complex
Fungal
|
Cancer
Infection
|
Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity.
|
-
- HY-N2177
-
3-Dehydrotrametenolic acid
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
|
-
- HY-N7069
-
4-Isopropylbenzyl alcohol
|
Others
|
Cancer
|
4-Isopropylbenzyl alcohol is a chemical composition of the essential oils from the leaves and flowers of Camellia nitidissima. C. nitidissima possess multiple biological activities including antioxidant activity, anticancer activity, and cytotoxicity as well as inhibiting the formation of advanced glycation end-products.
|
-
- HY-106784
-
Ajoene
|
Fungal
Apoptosis
|
Cancer
Infection
|
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities.
|
-
- HY-N2127
-
Pinostrobin
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Pinostrobin is a flavonoid can be found in many plants, and has anti-oxidant, anti-inflammatory, anti-cancer and neuroprotective properties. Pinostrobin is a potent PCSK9 inhibitor and inhibits the catalytic activity of PCSK9. Pinostrobin is a promising agent for cholesterol regulation and lipid management.
|
-
- HY-144088
-
ZYF0033
HPK1-IN-22
|
MAP4K
|
Cancer
Inflammation/Immunology
|
ZYF0033 (HPK1-IN-22, compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 decreases the phosphorylation of SLP76 (serine 376). ZYF0033 promotes anticancer immune responses. ZYF0033 inhibits tumor growth and caused increases intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells but decreased infiltration of regulatory T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells in the 4T-1 syngeneic mouse model.
|
-
- HY-N7148
-
γ-Tocopherol
D-γ-Tocopherol; (+)-γ-Tocopherol
|
COX
|
Cancer
Inflammation/Immunology
|
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
|
-
- HY-129578
-
-
- HY-103385
-
NCX4040
NO-Aspirin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
NCX4040 (NO-Aspirin), a non-steroidal anti-inflammatory drug (NSAID), is a nitric oxide (NO) releasing form of Aspirin. NCX4040 induces apoptosis in PC3 metastatic prostate cancer cells. NCX4040 has anti-inflammatory and anti-cancer effects.
|
-
- HY-120856
-
-
- HY-14289A
-
Cimetidine hydrochloride
SKF-92334 hydrochloride
|
Histamine Receptor
|
Cancer
Endocrinology
|
Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity.
|
-
- HY-N3354
-
Lupiwighteone
8-prenylgenistein
|
Apoptosis
|
Cancer
|
Lupiwighteone is an isoflavone present widely in wild-growing plants, with antioxidant, antimicrobial and anticancer effects. Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway.
|
-
- HY-B0302
-
Etidronic acid
Etidronate; HEDPA; HEDP
|
Apoptosis
|
Cancer
Metabolic Disease
|
Etidronic acid (Etidronate) is an orally and intravenously active bisphosphonate. Etidronic acid inhibits resorption of bone, reduces arterial calcification and can be used for osteoporosis research. Etidronic acid has anticancer activity. Etidronic acid is a chelating agent and can be used to remove heavy metal in water.
|
-
- HY-144841
-
CFT7455
|
Ligands for E3 Ligase
|
Cancer
|
CFT7455 is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. CFT7455 is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1).
|
-
- HY-D0226
-
Quinizarin
1,4-Dihydroxyanthraquinone
|
DNA/RNA Synthesis
Fungal
|
Cancer
Infection
|
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
|
-
- HY-126325
-
BY27
|
Epigenetic Reader Domain
|
Cancer
|
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity.
|
-
- HY-14289
-
Cimetidine
SKF-92334
|
Histamine Receptor
|
Cancer
Endocrinology
|
Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine has anti-cancer and anti-inflammatory activity.
|
-
- HY-N7044
-
-
- HY-114668
-
Camptothecin-20(S)-O-propionate
Camptothecin-20-O-propionate
|
Topoisomerase
|
Cancer
|
Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.
|
-
- HY-12412
-
ML132
NCGC-00183434
|
Caspase
|
Cancer
Inflammation/Immunology
|
ML132 (NCGC-00183434) is a selective caspase 1 inhibitor with an IC50 of 34.9 nM. ML132 shows good stability that can be utilized as molecular probes of caspase 1. ML132 can be used for research in the field of anti-cancer and anti-inflammatory.
|
-
- HY-147930
-
ACC1/2-IN-1
|
Acetyl-CoA Carboxylase
|
Cancer
|
ACC1/2-IN-1 (compound 4s) is a potent ACC1/2 inhibitor with IC50 values of 98.06 and 29.43 nM for ACC1 and ACC2, respectively. ACC1/2-IN-1 can be used for cancer research.
|
-
- HY-147716
-
CDK8-IN-6
|
CDK
|
Cancer
|
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer.
|
-
- HY-137977
-
DMU-212
|
ERK
Apoptosis
|
Cancer
|
DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.
|
-
- HY-128712
-
NCGC00029283
|
DNA/RNA Synthesis
|
Cancer
|
NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively.
|
-
- HY-50767S
-
Palbociclib-d8
PD 0332991-d8
|
CDK
|
Cancer
|
Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
|
-
- HY-147813
-
-
- HY-147932
-
ACC1/2-IN-2
|
Acetyl-CoA Carboxylase
|
Cancer
|
ACC1/2-IN-2 (compound PF-3) is a potent ACC1/2 inhibitor with IC50 values of 22 and 48 nM for ACC1 and ACC2, respectively. ACC1/2-IN-2 has antiproliferation activity and can be used for cancer research.
|
-
- HY-N7674A
-
Angoline hydrochloride
|
STAT
|
Cancer
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-118874
-
Oblimersen
|
Bcl-2 Family
Apoptosis
|
Cancer
|
Oblimersen is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen can be used for cancer research.
|
-
- HY-149011
-
CA IX-IN-1
|
Carbonic Anhydrase
|
Cancer
|
CA IX-IN-1 (compound 12g) is an effective and selective inhibitor of hCA IX with IC50 value of 7 nM. CA IX-IN-1 exhibits antitumor activity.
|
-
- HY-108992
-
Deoxynyboquinone
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Deoxynyboquinone, an excellent NQO1 substrate, is a potent antineoplastic agent. Deoxynyboquinone induces apoptosis in cancer cell lines. Deoxynyboquinone kills cancer cells through oxidative stress and reactive oxygen species (ROS) formation.
|
-
- HY-147928
-
Apoptotic agent-2
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research.
|
-
- HY-103440
-
EGFR/ErbB-2/ErbB-4 inhibitor-3
|
EGFR
|
Cancer
|
EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively.
|
-
- HY-147717
-
CDK8-IN-7
|
CDK
|
Cancer
|
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer.
|
-
- HY-124696
-
PU139
|
Histone Acetyltransferase
|
Cancer
|
PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
|
-
- HY-P3277
-
KRpep-2d
|
Ras
|
Cancer
|
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research.
|
-
- HY-147829
-
hCAXII-IN-2
|
Carbonic Anhydrase
|
Cancer
|
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II.
|
-
- HY-120337
-
V-11-0711
|
Others
|
Cancer
|
V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells.
|
-
- HY-139156
-
SK-575
|
PROTACs
PARP
|
Cancer
|
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC50 values of 19 ± 6 nM and 56 ± 12 nM, respectively.
|
-
- HY-106594A
-
Prussian blue insoluble
Iron(III) ferrocyanide; Milori blue
|
Bacterial
|
Cancer
Infection
Others
|
Prussian blue insoluble (Iron(III) ferrocyanide) is a good adsorbent to be used as antidotes for poisoning with cesium or thallium ions. Prussian blue insoluble (Iron(III) ferrocyanide) has anticancerous and antibacterial properties. Prussian blue insoluble (Iron(III) ferrocyanide) can be used as a contrast agent in photoacoustic and magnetic resonance imaging (MRI). Prussian blue insoluble can be used for contrast agents, antidotes and cancer research.
|
-
- HY-123578
-
NSC689857
|
EGFR
E1/E2/E3 Enzyme
|
Cancer
|
NSC689857 is a potent EGFR and SCF SKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others.
|
-
- HY-147839
-
Topoisomerase II inhibitor 10
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
|
-
- HY-N7674
-
Angoline
|
STAT
|
Cancer
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-B1799
-
Tolmetin
|
COX
|
Cancer
Inflammation/Immunology
|
Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID).
|
-
- HY-147929
-
Apoptotic agent-3
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research.
|
-
- HY-B1489
-
-
- HY-146792
-
PLK1-IN-4
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
|
-
- HY-N0523A
-
-
- HY-50898C
-
Lapatinib tosylate
GW572016 tosylate; GW2016 tosylate
|
EGFR
Ferroptosis
Autophagy
|
Cancer
|
Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
|
-
- HY-146724
-
Dot1L-IN-7
|
Histone Methyltransferase
|
Cancer
|
Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells.
|
-
- HY-146494
-
Androgen receptor antagonist 5
|
Androgen Receptor
|
Cancer
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer.
|
-
- HY-131055
-
Mytoxin B
|
ADC Cytotoxin
PI3K
Apoptosis
|
Cancer
|
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
|
-
- HY-124760
-
hSMG-1 inhibitor 11e
|
mTOR
PI3K
CDK
|
Cancer
|
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
|
-
- HY-143490
-
PAK4-IN-2
|
PAK
Apoptosis
|
Cancer
|
PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer.
|
-
- HY-P3277A
-
KRpep-2d TFA
|
Ras
|
Cancer
|
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research.
|
-
- HY-147983
-
PI3Kα-IN-8
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis.
|
-
- HY-147902
-
VEGFR-2-IN-24
|
VEGFR
|
Cancer
|
VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor with IC50 value of 0.22 µM. VEGFR-2-IN-24 can be used for tumor research.
|
-
- HY-D0254
-
Gallein
Pyrogallol phthalein
|
Others
|
Cancer
|
Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.
|
-
- HY-P99114
-
Sugemalimab
|
PD-1/PD-L1
|
Cancer
|
Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research.
|
-
- HY-N0711
-
-
- HY-130001
-
CDK9-IN-9
|
CDK
|
Cancer
|
CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
|
-
- HY-144448
-
FAK-IN-2
|
FAK
Apoptosis
|
Cancer
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
|
-
- HY-13649
-
Indibulin
ZIO 301; D 24851
|
Microtubule/Tubulin
Apoptosis
|
Cancer
Neurological Disease
|
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
|
-
- HY-10448S1
-
Capsaicin-d3
(E)-Capsaicin-d3
|
TRP Channel
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
Capsaicin-d3 ((E)-Capsaicin-d3) is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects.
|
-
- HY-78131A
-
(S)-(+)-Ibuprofen
(S)-Ibuprofen
|
COX
|
Inflammation/Immunology
|
(S)-(+)-Ibuprofen ((S)-Ibuprofen), a S(+)-enantiomer of Ibuprofen, is a potent COX-1 and COX-2 inhibitor with IC50s of 2.1 μM and 1.6 μM, respectively. (S)-(+)-Ibuprofen has analgesic, anti-inflammatory, anticancer and antipyretic effects.
|
-
- HY-N0328
-
-
- HY-146096
-
RMS3
|
P-glycoprotein
Apoptosis
|
Cancer
|
RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property.
|
-
- HY-126940
-
Furanodiene
|
Reactive Oxygen Species
P-glycoprotein
Apoptosis
|
Cancer
|
Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level.
|
-
- HY-123242A
-
FTI-2153 TFA
|
Farnesyl Transferase
|
Cancer
|
FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
|
-
- HY-15375
-
Allitinib
AST-1306; ALS 1306
|
EGFR
|
Cancer
|
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.
|
-
- HY-12035
-
AMG-208
|
c-Met/HGFR
Cytochrome P450
|
Cancer
|
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity.
|
-
- HY-17393S
-
Carboplatin-d4
NSC 241240-d4
|
DNA Alkylator/Crosslinker
Autophagy
DNA/RNA Synthesis
|
Cancer
|
Carboplatin-d4 (NSC 241240-d4) is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
|
-
- HY-108474
-
Nolatrexed dihydrochloride
AG 337; Thymitaq
|
Thymidylate Synthase
|
Cancer
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity.
|
-
- HY-118672
-
HNHA
|
HDAC
MMP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer.
|
-
- HY-141438
-
SIM1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.
|
-
- HY-N5086
-
-
- HY-128579
-
DW14800
|
Histone Methyltransferase
|
Cancer
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
|
-
- HY-125331
-
DRF-1042
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
|
-
- HY-141476
-
PI3K/mTOR Inhibitor-3
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity.
|
-
- HY-N0611
-
alpha-Boswellic acid
α-Boswellic acid
|
Others
|
Inflammation/Immunology
|
alpha-Boswellic acid (α-Boswellic acid) is a pentacyclic triterpene compound from extracts of Frankincense, has anticonvulsant and anti-cancer properties. alpha-Boswellic acid prevents and decreases the progression of Alzheimer’s hallmarks in vivo and can be used for Alzheimer’s disease research.
|
-
- HY-136541
-
YB-0158
Wnt pathway inhibitor 2
|
Wnt
Apoptosis
|
Cancer
|
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities.
|
-
- HY-125292
-
-
- HY-N3963
-
-
- HY-N0877
-
Bufalin
|
Na+/K+ ATPase
|
Cancer
|
Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
|
-
- HY-139385A
-
MPEG-2000-DSPE sodium
|
Parasite
|
Cancer
|
MPEG-2000-DSPE sodium is a phospholipid PEG conjugate, has both hydrophilicity and hydrophobility. MPEG-2000-DSPE sodium is used in the synthesis of liposomes, increases the hydrophilicity on the surface of liposomes, consequently increasing the longevity of liposomes in the blood circulation for the study of anticancer and antimalarial agents.
|
-
- HY-D0713
-
7ACC2
|
Monocarboxylate Transporter
Mitochondrial Metabolism
|
Cancer
|
7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [ 14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux.
|
-
- HY-123847
-
KPT-6566
|
Others
|
Cancer
|
KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
|
-
- HY-136144
-
FIDAS-5
|
Others
|
Cancer
|
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities.
|
-
- HY-139385
-
MPEG-2000-DSPE
|
|
Cancer
|
MPEG-2000-DSPE is a phospholipid PEG conjugate, has both hydrophilicity and hydrophobility. MPEG-2000-DSPE is used in the synthesis of liposomes, increases the hydrophilicity on the surface of liposomes, consequently increasing the longevity of liposomes in the blood circulation for the study of anticancer and antimalarial agents.
|
-
- HY-136342
-
Antitumor agent-23
|
Others
|
Cancer
|
Antitumor agent-23 is a potent anti-cancer agent with GI50s of 38, 48, 5, 27, 80, and 28 nM for lymphoma cell line GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI, respectively. Antitumoral activity.
|
-
- HY-13630
-
-
- HY-N1677
-
2,6-Dimethoxy-1,4-benzoquinone
|
Bacterial
Parasite
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
2,6-Dimethoxy-1,4-benzoquinone, a natural phytochemical, is a known haustorial inducing factor. 2,6-Dimethoxy-1,4-benzoquinone exerts anti-cancer, anti-inflammatory, anti-adipogenic, antibacterial, and antimalaria effects.
子
|
-
- HY-13427
-
Allitinib tosylate
AST-1306 (TsOH)
|
EGFR
|
Cancer
|
Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
|
-
- HY-136128
-
H3B-120
|
Potassium Channel
|
Cancer
|
H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
|
-
- HY-N6746
-
Citrinin
NSC 186
|
Bacterial
Fungal
|
Cancer
Infection
Neurological Disease
|
Citrinin is a mycotoxin which causes contamination in the food and is associated with different toxic effects. Citrinin is usually found together with another nephrotoxic mycotoxin, Ochratoxin A. Citrinin is also reported to possess a broad spectrum of bioactivities, including antibacterial, antifungal, and potential anticancer and neuro-protective effects in vitro.
|
-
- HY-132168
-
RMC-5552
|
mTOR
|
Cancer
|
RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.
|
-
- HY-N1416
-
Pogostone
|
Bacterial
Apoptosis
Autophagy
|
Infection
Inflammation/Immunology
|
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy.
|
-
- HY-B0335
-
Tolfenamic Acid
GEA 6414
|
COX
|
Inflammation/Immunology
Cancer
|
Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
|
-
- HY-126324
-
IV-23
|
Apoptosis
|
Cancer
|
IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
|
-
- HY-10218
-
Everolimus
RAD001; SDZ-RAD
|
mTOR
FKBP
Autophagy
Apoptosis
|
Cancer
|
Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
|
-
- HY-N10447
-
Kurzipene D
|
Apoptosis
|
Cancer
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration.
|
-
- HY-N6005
-
Methyl caffeate
|
Bacterial
|
Cancer
Infection
|
Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines.
|
-
- HY-N0808S
-
Camphor-d6
(±)-Camphor-d6
|
TRP Channel
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
Camphor-d6 ((±)-Camphor-d6) is the deuterium labeled Camphor. Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities. Camphor is a TRPV3 agonist.
|
-
- HY-120075
-
TJ191
|
Apoptosis
|
Cancer
|
TJ191 is a potent and specific anti-cancer agent that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. TJ191 has no affects on the proliferation of other cancer cells or normal fibroblasts or immune cells. TJ191 can be used for cancer research.
|
-
- HY-N10355
-
27-TBDMS-4-Dehydrowithaferin A
|
Apoptosis
|
Cancer
|
27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent.
|
-
- HY-10262
-
-
- HY-N0201
-
Atractylenolide I
|
Toll-like Receptor (TLR)
JAK
STAT
|
Cancer
|
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
|
-
- HY-115999
-
Carbonic anhydrase inhibitor 12
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
|
-
- HY-10253
-
AG1024
Tyrphostin AG 1024
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
|
-
- HY-119917
-
Gossypetin
|
p38 MAPK
MEK
Bacterial
|
Cancer
Infection
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
|
-
- HY-117113
-
JI051
|
Notch
|
Cancer
|
JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity.
|
-
- HY-N8309
-
-
- HY-B0302A
-
Etidronic acid disodium
Etidronate disodium; HEDPA disodium; HEDP disodium
|
Apoptosis
|
Cancer
Metabolic Disease
|
Etidronic acid (Etidronate) disodium is an orally and intravenously active bisphosphonate. Etidronic acid disodium inhibits resorption of bone, reduces arterial calcification and can be used for osteoporosis research. Etidronic acid disodium has anticancer activity. Etidronic acid disodium is a chelating agent and can be used to remove heavy metal in water.
|
-
- HY-B2099
-
Buformin
1-Butylbiguanide
|
AMPK
|
Cancer
Metabolic Disease
|
Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-B0114S1
-
Oxcarbazepine-d4-1
GP 47680-d4-1
|
Sodium Channel
Apoptosis
|
Cancer
Neurological Disease
|
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.
|
-
- HY-N0446
-
10-Methoxycamptothecin
|
Others
|
Cancer
|
10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and has been confirmed to possess high anti-cancer properties. 10-Methoxycamptothecin has higher cytotoxicity than 10-hydroxycamptothecin by testing antitumor activity against 2774 cell lines.
|
-
- HY-N0162
-
Luteolin
Luteoline; Luteolol; Digitoflavone
|
Keap1-Nrf2
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
|
-
- HY-B2099A
-
Buformin hydrochloride
1-Butylbiguanide hydrochloride
|
AMPK
|
Cancer
|
Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-P1954
-
Piscidin-1 (22-42)
|
Bacterial
|
Cancer
Infection
|
Piscidin-1 (22-42) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
|
-
- HY-136145
-
FIDAS-3
|
Wnt
|
Cancer
|
FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.
|
-
- HY-N0928
-
Mimosine
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Mimosine, a tyrosine analog , can act as an antioxidant by its potent iron-binding activity. Mimosine is a known chelator of Fe(III). Mimosine induces apoptosis through metal ion chelation, mitochondrial activation and ROS production in human leukemic cells. Anti-cancer, antiinflammation.
|
-
- HY-115470
-
CLK-IN-T3
|
CDK
DYRK
|
Cancer
|
CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
|
-
- HY-18366A
-
RU-SKI 43 hydrochloride
|
Hedgehog
|
Cancer
|
RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity.
|
-
- HY-18366
-
RU-SKI 43
|
Hedgehog
|
Cancer
|
RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity.
|
-
- HY-135336S
-
(R)-Verapamil D7 hydrochloride
(R)-(+)-Verapamil D7 hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
|
-
- HY-B0294
-
Flubendazole
|
Parasite
Microtubule/Tubulin
Apoptosis
|
Cancer
Infection
|
Flubendazole is a safe and efficacious anthelmintic drug, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle.
|
-
- HY-147977
-
ALR1/2-IN-1
|
Aldose Reductase
|
Cancer
|
ALR1/2-IN-1 (Compound 6e) is an aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitor with IC50 values of 3.26 μM and 3.06 μM against ALR1 and ALR2, respectively. ALR1/2-IN-1 shows anticancer activity.
|
-
- HY-14443
-
XMD8-92
|
ERK
Epigenetic Reader Domain
|
Cancer
|
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.
|
-
- HY-111549
-
Bragsin1
|
Others
|
Cancer
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
|
-
- HY-123952
-
RTC-5
TRC-382
|
EGFR
|
Cancer
|
RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
|
-
- HY-13630A
-
Etoposide phosphate disodium
BMY-40481 disodium
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
Neurological Disease
|
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-107856
-
5-Fluorouridine
|
Others
|
Cancer
|
5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
|
-
- HY-144650
-
Hsp90-Cdc37-IN-3
|
Apoptosis
HSP
|
Cancer
|
Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis.
|
-
- HY-W054146
-
RAMB4
|
Proteasome
|
Cancer
|
RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
|
-
- HY-N8481
-
3,6-Dihydroxyflavone
3,6-DHF
|
Apoptosis
|
Cancer
|
3,6-Dihydroxyflavone is an anti-cancer agent. 3,6-Dihydroxyflavone dose- and time-dependently decreases cell viability and induces apoptosis by activating caspase cascade, cleaving poly (ADP-ribose) polymerase (PARP). 3,6-Dihydroxyflavone increases intracellular oxidative stress and lipid peroxidation.
|
-
- HY-N1986
-
Cucurbitacin D
|
HSP
|
Cancer
|
Cucurbitacin D is an active component in Cucurbita texana, disrupts interactions between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of the heat shock response. Anti-cancer activity.
|
-
- HY-N0794
-
Proanthocyanidins
|
Bacterial
Fungal
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
Proanthocyanidins are a class of polyphenolic that are widely distributed in higher plants, consisted of an electrophilic flavanyl unit. Proanthocyanidins can be used as antioxidant and anti-cancers agent. Proanthocyanidins also exhibit anti-inflammatory, cardioprotective, antibacterial and antifungal properties, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy..
|
-
- HY-N0664
-
Aucubin
|
Bacterial
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
Aucubin, an iridoid glucoside, is isolated from Plantago asiatica, Eucommia ulmoides, the leaves of Aucuba japonica and more recently from butterfly larva. Aucubin has many biological activities, such as antioxidant, anti-aging, anti-inflammatory, antimicrobial, anti-fibrotic, anti-cancer, hepatoprotective, neuroprotective and osteoprotective effects.
|
-
- HY-N2298
-
Camellianin A
|
Apoptosis
|
Cancer
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-N0817
-
Polyphyllin G
|
Apoptosis
Autophagy
Bacterial
|
Cancer
Inflammation/Immunology
|
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs).
Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
|
-
- HY-15287S
-
Nelfinavir-d3
|
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
|
-
- HY-130307
-
Rubrofusarin
|
Bacterial
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Rubrofusarin is an orange polyketide pigment from Fusarium graminearum. Rubrofusarin is also an active ingredient of the Cassia species and ameliorates chronic restraint stress (CRS) -induced depressive symptoms through PI3K/Akt signaling. Rubrofusarin has anticancer, antibacterial, and antioxidant effects.
|
-
- HY-139065
-
AMPC
|
Others
|
Cancer
|
AMPC is a potent and effective TFF3 inhibitor. AMPC inhibits cell proliferation, survival, oncogenicity, and CSC-like behaviour in TFF3-positive CMS4 CRC cells. AMPC acts as a potential anti-cancer agent alone or in combination with 5-FU, and can be used for cancer research.
|
-
- HY-N2208
-
4-Hydroxylonchocarpin
|
p38 MAPK
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities.
|
-
- HY-124596
-
CD161
NKR-P1A
|
Epigenetic Reader Domain
|
Cancer
|
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
|
-
- HY-P1954A
-
Piscidin-1 (22-42) (TFA)
|
Bacterial
|
Infection
|
Piscidin-1 (22-42) (TFA) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) (TFA) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
|
-
- HY-103319
-
Calmidazolium chloride
R 24571
|
CaMK
Autophagy
|
Cancer
Neurological Disease
|
Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
|
-
- HY-N1535
-
Ponicidin
Rubescensine B
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
|
-
- HY-147726
-
Microtubule inhibitor 5
|
Microtubule/Tubulin
|
Cancer
|
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability.
|
-
- HY-146305
-
-
- HY-143872
-
Bcl-2-IN-4
|
Bcl-2 Family
|
Cancer
|
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2).
|
-
- HY-101087
-
-
- HY-147520
-
-
- HY-149002
-
Topoisomerase I/II inhibitor 4
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
|
-
- HY-146197
-
Apoptotic agent-1
|
Apoptosis
|
Cancer
|
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes.
|
-
- HY-100002
-
-
- HY-146660
-
BRD4 Inhibitor-18
|
c-Myc
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity.
|
-
- HY-100549
-
(S)-Crizotinib
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.
|
-
- HY-107209
-
RKI-1313
|
ROCK
|
Cancer
|
RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth.
|
-
- HY-146472
-
EGFR-IN-52
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis.
|
-
- HY-147935
-
NTQ1062
|
Akt
|
Cancer
|
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model.
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- HY-146061
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KRAS G12C inhibitor 48
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Ras
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Cancer
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KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively.
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- HY-146114
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Antitumor agent-67
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Others
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Cancer
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Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity.
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- HY-131203
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PROTAC BRD4 Degrader-6
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Epigenetic Reader Domain
Apoptosis
c-Myc
Caspase
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Cancer
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PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research.
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- HY-P99010
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Bemarituzumab
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FGFR
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Cancer
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Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research.
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- HY-147698
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ZLHQ-5f
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CDK
Topoisomerase
Apoptosis
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Cancer
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ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
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- HY-132296
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GSK215
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FAK
PROTACs
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Cancer
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GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
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- HY-139353
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- HY-146136
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EGFR-IN-56
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EGFR
Apoptosis
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Cancer
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EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis.
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- HY-147562
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- HY-145924
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BAY 2666605
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Phosphodiesterase (PDE)
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Cancer
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BAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135).
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- HY-N4058
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Helichrysetin
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Apoptosis
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Cancer
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Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
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- HY-147007
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