74

CX-5461

74 Publications Verification

Cat. No.: HY-13323

CAS No.: 1138549-36-6

Purity: 99.49%

Target:

DNA/RNA Synthesis MDM-2/p53 AMPK Akt Autophagy Apoptosis Checkpoint Kinase (Chk)

Research Areas:

Cancer

CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors .

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74

CX-5461 dihydrochloride

74 Publications Verification

Cat. No.: HY-13323A

Purity: 99.41%

Target:

DNA/RNA Synthesis MDM-2/p53 AMPK Akt Autophagy Apoptosis Checkpoint Kinase (Chk)

Research Areas:

Cancer

CX-5461 dihydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 dihydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 dihydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 dihydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 dihydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors .

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57

Ulixertinib hydrochloride

57 Cited Publications

Cat. No.: HY-15816A

CAS No.: 1956366-10-1

Purity: 99.89%

Synonyms: BVD-523 hydrochloride; VRT752271 hydrochloride

Target:

ERK

Research Areas:

Cancer

Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

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57

Ulixertinib

57 Cited Publications

Cat. No.: HY-15816

CAS No.: 869886-67-9

Purity: 99.95%

Synonyms: BVD-523; VRT752271

Target:

ERK

Research Areas:

Cancer

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

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28

PD 169316

28 Cited Publications

Cat. No.: HY-10578

CAS No.: 152121-53-4

Purity: 98.29%

Target:

p38 MAPK Autophagy Enterovirus

Research Areas:

Cancer

PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC₅₀ of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.

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12

NHC-triphosphate tetraammonium

12 Cited Publications

Cat. No.: HY-135867E

Purity: 97.09%

Target:

CHIKV Endogenous Metabolite Enterovirus HCV Topoisomerase SARS-CoV

Research Areas:

Infection

NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form . NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA .

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10

TAS4464

10 Cited Publications

Cat. No.: HY-128586

CAS No.: 1848959-10-3

Purity: 99.52%

Target:

Apoptosis Carbonic Anhydrase NEDD8-activating Enzyme

Research Areas:

Cancer

TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC₅₀=0.955 nM), and also inhibits CAII with an IC₅₀ of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC₅₀ values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .

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10

TAS4464 hydrochloride

10 Cited Publications

Cat. No.: HY-128586A

CAS No.: 1848959-11-4

Purity: 98.91%

Target:

NEDD8-activating Enzyme Carbonic Anhydrase Apoptosis

Research Areas:

Cancer

TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC₅₀=0.955 nM), and also inhibits CAII with an IC₅₀ of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC₅₀ values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .

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6

Gartisertib

6 Cited Publications

Cat. No.: HY-136270

CAS No.: 1613191-99-3

Purity: 99.77%

Synonyms: VX-803; M4344; ATR inhibitor 2

Target:

ATM/ATR

Research Areas:

Cancer

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a K_i of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC₅₀ of 8 nM. Antitumor activity .

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