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Results for "

PARP inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PARP (18) Akt (2) Antibiotic (1) Apoptosis (10) Autophagy (2) Bcl-2 Family (2) c-Myc (1) Caspase (2) Deubiquitinase (1) NF-κB (1) P-glycoprotein (2) p38 MAPK (2) RAD51 (1) Topoisomerase (1)
By Research Areas:	Cancer (19) Inflammation/Immunology (2) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Targets Recommended: PARP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148754

PARP10-IN-3	PARP	Cancer
PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase *PARP10* inhibitor with an IC₅₀ of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on *PARP2* and *PARP15* with IC₅₀s of 1.7 μM for human PARP2 and human PARP15, respectively .

HY-147886

PARP1-IN-11	PARP	Cancer
PARP1-IN-11 (compound 49) is a potent *PARP1* inhibitor with IC₅₀ value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .

HY-148753

PARP10-IN-2	PARP	Cancer
PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase *PARP10* inhibitor with an IC₅₀ of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on *PARP2* and *PARP15* with IC₅₀s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively .

HY-164926

PARP1-IN-33	PARP	Neurological Disease
PARP1-IN-33 (Example 6) is a *PARP1* inhibitor (IC₅₀: 0.41 nM). PARP1-IN-33 has retinal cytoprotective effect, with an EC₅₀ of 0.02 nM (inhibition on MTS activity of H₂O₂ induced human retinal pigment epithelial cell) .

HY-10619B

Niraparib tosylate Maximum Cited Publications 64 Publications Verification MK-4827 tosylate	PARP Apoptosis	Cancer
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable *PARP1* and *PARP2* inhibitor with an IC₅₀ of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-10619E

Niraparib tosylate hydrate Maximum Cited Publications 64 Publications Verification MK-4827 tosylate hydrate	PARP Apoptosis	Cancer
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable *PARP1* and *PARP2* inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-15050

KCL-440	PARP	Neurological Disease Inflammation/Immunology
KCL-440 is a CNS-penetrated *PARP* inhibitor, with an IC₅₀ of 68 nM. KCL-440 has strong inhibition of PARP-1 .

HY-168094

PARP1-IN-30	PARP	Cancer
PARP1-IN-30 (Compound 3) is a specific and potent *PARP1* inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of *PARP1* in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .

HY-158138

TOPOI/PARP-1-IN-1	PARP Topoisomerase Apoptosis	Cancer
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic *TOPOI/PARP* dual inhibitor with an IC₅₀ value of 0.09 μM for *PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit* the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .

HY-162104

BRCA2-RAD51-IN-1	RAD51	Cancer
BRCA2-RAD51-IN-1 (Compound 46) is a BRCA2-RAD51 inhibitor with an EC₅₀ value of 28 μM. BRCA2-RAD51-IN-1 has antitumor activity .

HY-10619

Niraparib Maximum Cited Publications 64 Publications Verification MK-4827	PARP Apoptosis	Cancer
Niraparib (MK-4827) is a highly potent and orally bioavailable *PARP1* and *PARP2* inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-10619A

Niraparib hydrochloride Maximum Cited Publications 64 Publications Verification MK-4827 hydrochloride	PARP Apoptosis	Cancer
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable *PARP1* and *PARP2* inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

HY-115552

Simmiparib	PARP	Cancer
Simmiparib is a highly potent and orally active *PARP1* and *PARP2* inhibitor with IC₅₀ values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .

HY-10619R

Niraparib (Standard)	PARP Apoptosis	Cancer
Niraparib (Standard) is the analytical standard of Niraparib. This product is intended for research and analytical applications. Niraparib (MK-4827) is a highly potent and orally bioavailable *PARP1* and *PARP2* inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .

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-130073

Amorfrutin A	NF-κB Apoptosis	Cancer
Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .

HY-13968

JW 55 3 Publications Verification	PARP	Cancer
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC₅₀s of 1.9 μM and 830 nM respectively.

HY-N3584

Paris saponin VII 3 Publications Verification Chonglou Saponin VII	Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis	Cancer
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of *Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt*. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .

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-N3584R

Paris saponin VII (Standard)	Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis	Cancer
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .

HY-16958R

PD 404182 (Standard)	Antibiotic	Inflammation/Immunology
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .

HY-162633

USP1-IN-9	Deubiquitinase	Cancer
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC₅₀ of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .

Paris saponin VII 3 Publications Verification Chonglou Saponin VII	Structural Classification Liliaceae Classification of Application Fields Source classification Trillium tschonoskii Maxim. Plants Disease Research Fields Steroids Cancer	Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of *Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt*. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .

Amorfrutin A	Structural Classification Simple Phenylpropanols Leguminosae Source classification Amorpha fruticosaL. Phenylpropanoids Plants	NF-κB Apoptosis
Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .

Paris saponin VII (Standard)	Structural Classification Liliaceae Source classification Trillium tschonoskii Maxim. Plants Steroids	Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .

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PARP inhibition

Inhibitors & Agonists

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