Search Result

Results for "

regression

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (1) Apoptosis (7) Autophagy (1) Btk (1) Cathepsin (1) CCR (1) CD20 (1) CD3 (1) Checkpoint Kinase (Chk) (1) CXCR (1) EGFR (2) Epigenetic Reader Domain (4) Estrogen Receptor/ERR (1) Farnesyl Transferase (1) FGFR (4) Fluorescent Dye (1) Galectin (1) Histone Methyltransferase (1) HSP (1) IFNAR (1) IRAK (1) Microtubule/Tubulin (3) mTOR (1) PDGFR (3) PI3K (3) PROTACs (6) Ras (4) ROS Kinase (1) STAT (3) STING (4) TNF Receptor (1) VEGFR (1)
By Research Areas:	Cancer (47) Infection (2) Inflammation/Immunology (4)

By Targets:

AMPK (1)

Anaplastic lymphoma kinase (ALK) (1)

Androgen Receptor (1)

Apoptosis (7)

Autophagy (1)

Btk (1)

Cathepsin (1)

CCR (1)

CD20 (1)

CD3 (1)

Checkpoint Kinase (Chk) (1)

CXCR (1)

EGFR (2)

Epigenetic Reader Domain (4)

Estrogen Receptor/ERR (1)

Farnesyl Transferase (1)

FGFR (4)

Fluorescent Dye (1)

Galectin (1)

Histone Methyltransferase (1)

HSP (1)

IFNAR (1)

IRAK (1)

Microtubule/Tubulin (3)

mTOR (1)

PDGFR (3)

PI3K (3)

PROTACs (6)

Ras (4)

ROS Kinase (1)

STAT (3)

STING (4)

TNF Receptor (1)

VEGFR (1)

By Research Areas:

Cancer (47)

Infection (2)

Inflammation/Immunology (4)

Inhibitors & Agonists

Biochemical Assay Reagents

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114277

Sotorasib Maximum Cited Publications 44 Publications Verification AMG-510	Ras	Cancer
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors .

HY-13479

EC144	HSP	Cancer
EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC₅₀ of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-160047

AX102 sodium	PDGFR	Cancer
AX102 sodium is a 34 bp length nucleotide aptamer modified at the 5' end with a 40 kDa polyethylene glycol moiety. AX102 selectively binds platelet-derived growth factor B (PDGF-B) and causes tumor vessel regression .

HY-160048

PEG40K unconjugated/naked AX102 sodium	PDGFR	Cancer
PEG40K unconjugated/naked AX102 sodium is AX102 without PEG40K conjugation. AX102 is a DNA oligonucleotide aptamer for platelet-derived growth factor PDGF-B. AX102 is 34 bases in length, selectively binds platelet-derived growth factor B (PDGF-B), and causes tumor vessel regression .

HY-161373

PI3Kα-IN-22	PI3K	Cancer
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα ^H1047R, with an IC₅₀ of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .

HY-145734A

AMXI-5001 hydrochloride	Microtubule/Tubulin	Cancer
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC₅₀s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .

HY-145734

AMXI-5001	Microtubule/Tubulin	Cancer
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC₅₀s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .

HY-148029

Dazostinag disodium TAK-676	STING	Cancer
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .

HY-143881

FGFR4-IN-6	FGFR	Cancer
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC₅₀ value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-132234

M-1211	Epigenetic Reader Domain	Cancer
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression .

HY-12885

ADU-S100 MIW815; ML RR-S2 CDA	STING	Inflammation/Immunology Cancer
ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .

HY-132922

EEDi-5273 APG-5918	Histone Methyltransferase	Cancer
EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC₅₀ = 0.2 nM) capable of achieving complete and persistent tumor regression.

HY-W035051

TSPP tetrasodium	Fluorescent Dye	Infection Cancer
TSPP tetrasodium is a photosensitizer that has shown impressive effects in in vivo regression of cancer and microorganism infections (Ex: 413 nm, Em: 640 nm) .

HY-12885B

ADU-S100 ammonium salt 40+ Cited Publications MIW815 ammonium salt; ML RR-S2 CDA ammonium salt	STING	Inflammation/Immunology Cancer
ADU-S100 ammonium salt (MIW815 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .

HY-136447

ASP4132 1 Publications Verification	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-114228

PROTAC BET degrader-2 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC₅₀ value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.

HY-111145

RD162	Androgen Receptor	Cancer
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .

HY-156681

STX-478	PI3K	Cancer
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .

HY-110201

Estrogen receptor modulator 1	Estrogen Receptor/ERR	Cancer
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC₅₀ of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .

HY-151559

Zn-DPA-maytansinoid conjugate 1	Checkpoint Kinase (Chk) STAT CXCR CCR	Cancer
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an “inflamed hot tumor” .

HY-17449

Fosbretabulin disodium CA 4DP; CA 4P; Combretastatin A4 disodium phosphate	Microtubule/Tubulin Apoptosis	Cancer
Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis .

HY-147250A

Lirafugratinib hydrochloride RLY-4008 hydrochloride	FGFR	Cancer
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-147250

Lirafugratinib RLY-4008	FGFR	Cancer
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-148274

KTX-582	PROTACs IRAK Apoptosis	Cancer
KTX-582 is a potent IRAK4 degrader with DC₅₀ values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88 ^MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model .

HY-114277S

Sotorasib-d7 AMG-510-d₇	Ras	Cancer
Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .

HY-P99776

Plamotamab XmAb-13676	CD20 CD3	Cancer
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 ⁺ expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .

HY-100765

BI-0252
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC₅₀ of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .

HY-144070

ErSO-DFP	Others	Cancer
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .

HY-10517A

(Z)-Orantinib (Z)-SU6668; (Z)-TSU-68	VEGFR PDGFR FGFR	Cancer
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors .

HY-101519

BETd-260 1 Publications Verification ZBC 260	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .

HY-119257

ABT-100	Farnesyl Transferase Apoptosis	Cancer
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC₅₀s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity .

HY-131909

CJ-2360	Anaplastic lymphoma kinase (ALK)	Cancer
CJ-2360 is a potent and orally active ALK inhibitor with IC₅₀s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .

HY-16231

GGTI-2418	ROS Kinase Apoptosis	Cancer
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC₅₀s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .

HY-155537

YK-029A	EGFR	Cancer
YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR ^T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .

HY-136360

MI-3454 2 Publications Verification	Epigenetic Reader Domain	Cancer
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC₅₀ of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .

HY-114440

Belapectin GR-MD-02	Galectin Apoptosis	Cancer
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity K_i of 2.8 μM .

HY-156498

RMC-7977	Ras	Cancer
RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRAS ^G12C cancer models .

HY-102087

JPM-OEt 3 Publications Verification	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .

HY-111373

RapaLink-1 5 Publications Verification	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-131328

Pirtobrutinib 1 Publications Verification LOXO-305	Btk	Cancer
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .

HY-136927

MSA-2 5+ Cited Publications	STING	Inflammation/Immunology Cancer
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC₅₀s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .

HY-145414

DYSP-C34	Others	Cancer
DYSP-C34 is a potent, biocompatible, and ultrasound (US)-triggered multifunctional molecular machine. DYSP-C34 has multiple favorable properties, such as improved lipophilic/hydrophilic balance, intensified US-induced ROS production capacity, and better cellular permeability, resulting in the excellent tumor target efficiency and notable sonodynamic therapy (SDT)-mediated tumor regression. DYSP-C34 exhibits mild immunogenicity by stimulating APCs directly .

HY-149695

EGFR-IN-91	EGFR	Cancer
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR ^L858R/C797S and EGFR ^{exon 19del/C797S}, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .

HY-148813

AK-2292	PROTACs STAT	Cancer
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC₅₀ of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-150725

ODN 1585	IFNAR TNF Receptor	Infection Inflammation/Immunology Cancer
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .

HY-149427

PI3Kα-IN-12	PI3K	Cancer
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC₅₀: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC₅₀s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .

HY-155356

YN14	PROTACs Ras	Cancer
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.

HY-129602

SD-36 5 Publications Verification	PROTACs STAT Apoptosis	Cancer
SD-36 is a potent and efficacious STAT3 PROTAC degrader (K_d=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC₅₀=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name	Category	Target	Chemical Structure