| DC48973 |
CPT-Se4 |
CPT-Se4, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM). |
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| DC48974 |
SKLB-197 |
SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo. |
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| DC48977 |
CDK6/PIM1-IN-1 |
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity. |
|
| DC49019 |
ATR-IN-10 |
ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC50 value of 2.978 μM. |
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| DC49031 |
ATR-IN-5 |
ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24). |
|
| DC49034 |
CDK9-IN-13 |
CDK9-IN-13 (compound 38) is potent and selective CDK9 inhibitor, with an IC50 of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents. |
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| DC49052 |
OM-153 |
OM-153 is a potent tankyrase inhibitor with IC50s of 13 and 2 nM for tankyrase 1 and tankyrase 2, respectively. OM-153 shows inhibition of WNT/β-catenin signaling and proliferation in COLO 320DM. |
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| DC49061 |
ATR-IN-6 |
ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22). |
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| DC49082 |
CDK5-IN-2
Featured
|
CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively. |
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| DC49543 |
ATR-IN-11 |
ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent drug discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease. |
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| DC49544 |
ATR-IN-12 |
ATR-IN-12 (Compound 5g) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with an IC50 value of 0.007 μM. ATR-IN-12 displays good anti-tumor activity and significantly reduces the phosphorylation level of ATR and its downstream signaling protein. ATR-IN-12 is a promising lead compound for subsequent drug discovery targeting ATR kinase. |
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| DC49545 |
Retreversine |
Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor. |
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| DC49546 |
Aurora kinase inhibitor-8 |
Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases. |
|
| DC49547 |
Aurora A/PKC-IN-1 |
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity. |
|
| DC49548 |
Aurora A inhibitor 1 |
Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A. Aurora A has been implicated in cancers of diverse histological origin and may possess oncogenic properties when overexpressed. Aurora A inhibitor 1 has the potential for the research of cancer diseases mediated by aurora a (extracted from patent WO2021147974A1, compound 49). |
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| DC49549 |
dAURK-4 |
dAURK-4, an Alisertib derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 has anticancer effects. |
|
| DC49550 |
Aurora kinase-IN-1 |
Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents. |
|
| DC49551 |
Aurora/LIM kinase-IN-1 |
Aurora/LIM kinase-IN-1 (Compound F114) is a potent and dual inhibitor of aurora and lim kinase. Aurora kinases and lim kinases are involved in neoplastic cell division and cell motility, respectively. Aurora/LIM kinase-IN-1 inhibits GBM proliferation and invasion. Aurora/LIM kinase-IN-1 is a promising new scaffold for dual aurora/lim kinase inhibitors that may be used in future drug development efforts for GBM, and potentially other cancers. |
|
| DC49552 |
dAURK-4 hydrochloride |
dAURK-4 hydrochloride, an Alisertib derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 hydrochloride has anticancer effects. |
|
| DC49553 |
(S)-CTX-712 |
(S)-CTX-712 （Example 287） is a novel splicing modulator. |
|
| DC49554 |
DENV-IN-4 |
DENV-IN-4 is a potent DENV inhibitor (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect. |
|
| DC49555 |
Pol I-IN-1 |
Pol I-IN-1 is a potent RNA polymerase I (Pol I) inhibitor with IC50 0.21 µM for the Pol I large catalytic subunit RPA194. |
|
| DC49556 |
CHIKV-IN-3 |
CHIKV-IN-3 is a potent against two low-passage CHIKV inhibitor with EC50 values of 1.55 and 0.14 µM for CHIKV-122508 and CHIKV-6708, respectively. CHIKV-IN-3 acts on the host cells to interfere with the viral replication. CHIKV-IN-3 displays minimal cytotoxic liability(CC50 > 100 µM). Prophylactic effect. |
|
| DC49557 |
DNA-PK-IN-6 |
DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of drug resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6). |
|
| DC49558 |
DNA-PK-IN-4 |
DNA-PK-IN-4 is a potent inhibitor of DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27). |
|
| DC49559 |
DNA-PK-IN-3 |
DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4). |
|
| DC49560 |
Bis-Pro-5FU |
Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer. |
|
| DC49561 |
NCT-TFP |
NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors (extracted from patent US20190331688A1). |
|
| DC49562 |
AZ3391 |
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23). |
|
| DC49563 |
PARP-1-IN-1 |
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model. |
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